P450 (e.g. CYP17)

P450 (e.g. CYP17)产品

  • 所有产品(89)
  • P450 (e.g. CYP17)抑制剂 (74)
  • P450 (e.g. CYP17)抗体 (3)
  • P450 (e.g. CYP17)激活剂 (4)
  • P450 (e.g. CYP17)调节剂 (2)
目录号 产品名 产品描述 文献引用 实验数据
S1185 Ritonavir Ritonavir是Cytochrome P450 3AHIV蛋白酶抑制剂,用于治疗HIV感染和AIDS。抑制Cytochrome P450 2D6, P-Glycoprotein,诱导Cytochrome P450 2C19, Cytochrome P450 1A2, Cytochrome P450 2C9, Cytochrome P450 2B6UDP Glucuronosyltransferases。Ritonavir 可诱导凋亡。
Cancer Drug Resist, 2024, 7:3
Int. J. Mol. Sci, 2023, 10.3390/ijms24076062
Int J Mol Sci, 2023, 24(7)6062
S2476 Itraconazole Itraconazole是一种三唑类抗真菌药物,是CYP3A4的有效抑制剂,IC50为6.1 nM。Itraconazole 是一个有效的Hedgehog (Hh)信号通路的拮抗剂。Itraconazole 可通过诱导自噬来抑制恶性胶质瘤的生长。
Front Cell Infect Microbiol, 2023, 13:1128000
Front Cell Infect Microbiol, 2022, 12:864912
Front Cell Infect Microbiol, 2022, 12:1074903
S1123 Abiraterone Abiraterone是一种有效CYP17抑制剂,无细胞试验中IC50为2 nM。Abiraterone (CB-7598) 是一种雄性激素 androgen 生物合成抑制剂。
Cancer Res, 2023, 83(8):1361-1380
Cancer Cell, 2021, S1535-6108(21)00659-0
Cancers (Basel), 2021, 13(16)3959
S2246 Abiraterone Acetate Abiraterone Acetate是Abiraterone的醋酸盐形式,是一种甾体类细胞色素CYP17抑制剂,无细胞试验中IC50为72 nM。Abiraterone acetateis 是一种口服的雄性激素 androgen 生物合成抑制剂。
Cancer Res, 2023, 83(2):219-238
J Immunother Cancer, 2023, 11(5)e006581
Pharmacol Res, 2023, 189:106692
S2262 Apigenin Apigenin是一种有效的CYP2C9抑制剂,Ki为2 μM.。
Transl Oncol, 2023, 35:101712
Molecules, 2023, 28(13)4947
Pharmacol Res, 2022, 185:106489
S2268 Baicalein Baicalein是CYP2C9和脯氨酰肽链内切酶抑制剂。
SLAS Discov, 2024, S2472-5552(24)00007-8
Redox Rep, 2023, 28(1):2152607
Microbiol Spectr, 2023, 11(3):e0470222
S1257 Posaconazole Posaconazole是CYP3A4的抑制剂,但不抑制其他CYP酶的活性;同时是sterol C14ɑ demethylase的抑制剂,IC50为0.25 μM。其平均的消除半衰期为15-35小时。
Front Cell Infect Microbiol, 2022, 12:1074903
Front Cell Infect Microbiol, 2022, 12:864912
Int J Mol Sci, 2022, 23(22)13809
S1442 Voriconazole Voriconazole是类似于氟康唑和伊曲康唑的新型三唑衍生物,其作用是通过抑制真菌 cytochrome P-450 依赖性的,14-alpha-sterol demethylase 介导的 麦角固醇的合成。
Front Cell Infect Microbiol, 2022, 12:864912
Front Cell Infect Microbiol, 2022, 12:1074903
Int J Mol Sci, 2022, 23(22)13809
S1331 Fluconazole Fluconazole是一种羊毛甾醇14 alpha去甲基化酶 抑制剂,抑制了麦角固醇的形成,用于治疗和预防浅表性和全身性真菌感染。
Front Cell Infect Microbiol, 2024, 14:1296151
Nat Commun, 2022, 13(1):1658
Nat Commun, 2022, 13(1):4295
S1353 Ketoconazole Ketoconazole能抑制cyclosporine oxidase(环孢素氧化酶)testosterone 6 beta-hydroxylase(睾丸素6β-羟化酶)IC50分别为0.19 mM和0.22 mM。Ketoconazole 是一种雄性激素 androgen 生物合成抑制剂。
J Med Virol, 2023, 95(6):e28856
Cell Death Dis, 2023, 14(1):64
Cell Death Dis, 2023, 14(8):488
S4202 Verapamil HCl Verapamil HCl是L-型钙通道抑制剂,是第四类抗心律失常的药剂。Verapamil 可抑制 permeability-glycoprotein (P-gp)CYP3A4
Cancers (Basel), 2023, 15(15)3774
EMBO Mol Med, 2022, 14(2):e14903
Cell Rep, 2022, 38(10):110468
S2187 Avasimibe Avasimibe 抑制ACATIC50为3.3 μM,也抑制人P450同工酶CYP2C9, CYP1A2和CYP2C19,IC50分别为2.9 μM, 13.9 μM和26.5 μM,
PLoS Pathog, 2023, 19(5):e1011323
Hepatol Int, 2023, 10.1007/s12072-023-10490-4
Front Pharmacol, 2022, 13:795934
S1712 Deferasirox Deferasirox是一种铁螯合剂,是cytochrome P450 3A4诱导剂,Cytochrome P450 2C8的抑制剂,Cytochrome P450 1A2抑制剂。Deferasirox 引起的铁损耗可促进BclxL下调和细胞死亡。
J Transl Med, 2023, 21(1):50
Cell Death Discov, 2023, 9(1):97
Cancer Discov, 2022, 12(9):2180-2197
S1794 Fenofibrate Fenofibrate是一种Fibrate类化合物,是纤维酸衍生物。Fenofibrate 是 PPARα 的选择性激动剂,EC50为30μM。Fenofibrate 可结合并抑制 cytochrome P450 epoxygenase (CYP)2C ,对于CYP2C19、CYP2B6和CYP2C9的IC50分别为0.2 μM、0.7 μM和9.7 μM。Fenofibrate 可诱导自噬。
Cancer Lett, 2023, 10.1016/j.canlet.2023.216427
Cell Metab, 2022, 34(2):299-316.e6
Cancers (Basel), 2022, 14(2)282
S2900 Cobicistat Cobicistat是一种有效的CYP3A选择性抑制剂,IC50为30 - 285 nM。
J Pers Med, 2022, 12(2)258
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Hum Cell, 2021, 34(6):1911-1918
S2046 Pioglitazone HCl Pioglitazone HCl (AD-4833, U-72107E) 是一种 cytochrome P450 (CYP)2C8CYP3A4 酶的抑制剂。Pioglitazone HCl 抑制CYP2C8、CYP3A4和CYP2C9的Ki值分别为1.7 μM、11.8 μM和32.1 μM。Pioglitazone HCl 也是一种选择性的 peroxisome proliferator-activated receptor-gamma (PPARγ) 激动剂,对人PPARγ和小鼠PPARγ的EC50值分别为0.93 μM和0.99 μM。Pioglitazone HCl 可抑制线粒体内铁的摄取、脂质过氧化和随后的铁死亡。
Commun Biol, 2022, 5(1):231
J Genet Genomics, 2022, S1673-8527(22)00133-3
J Cell Mol Med, 2022, 10.1111/jcmm.17154
S2394 Naringenin Naringenin (NSC 34875, S-Dihydrogenistein, NSC 11855, Salipurol)是来自于食用植物的一种天然的主要黄酮类化合物,有益人体健康,具有生物活性,是一种抗氧化剂,自由基清除剂,抗炎,碳水化合物代谢启动子及免疫系统的调制剂。
J Transl Med, 2024, 22(1):208
Molecules, 2023, 28(13)4947
Biomed Res Int, 2022, 2022:8080679
S4662 Atazanavir Atazanavir (Latazanavir, Zrivada, Reyataz, BMS-232632) 是一种氮杂肽及HIV-蛋白酶抑制剂,常与其他抗HIV药物结合,用于治疗HIV感染以及获得性免疫缺乏综合征。Atazanavir 是 cytochrome P450 isozyme 3A (CYP3A4) 的底物和抑制剂,也是 P-glycoprotein 的抑制剂和诱导剂。
Int J Mol Sci, 2022, 23(23)15380
Chemistry, 2022, e202202798.
Sci Rep, 2021, 11(1):19443
S1952 Methoxsalen Methoxsalen (Xanthotoxin, NCI-C55903) 是在一些植物中发现的天然存在的呋喃香豆素化合物,包括补骨脂,用于治疗牛皮癣,湿疹,白癜风及一些暴露在阳光下的皮肤淋巴瘤。是CYP2A5/6抑制剂。
J Pers Med, 2022, 12(2)258
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Hum Cell, 2021, 34(6):1911-1918
S2803 Galeterone Galeterone (TOK-001)是一种选择性CYP17抑制剂,也是androgen receptor (AR)(雄激素受体)拮抗剂,IC50分别为300 nM和384 nM,也有效抑制人类前列腺肿瘤生长。Phase 2。
ChemMedChem, 2022, e202200043
Cancer Chemother Pharmacol, 2020, 10.1007/s00280-020-04195-w
Steroids, 2020, 153:108534
S2555 Clarithromycin Clarithromycin (A-56268) 是一种大环内酯类抗生素,是CYP3A4抑制剂,用于治疗许多细菌感染。
Microorganisms, 2022, 10(7)1421
Cell Biol Toxicol, 2021, 10.1007/s10565-021-09646-5
J Ovarian Res, 2019, 12(1):107
S5658 Omeprazole Sodium Omeprazole Sodium is the sodium salt form of omeprazole, which is a proton pump inhibitor and suppresses gastric acid secretion. Omeprazole Sodium is a metabolism-dependent inhibitor (MDI) of CYP2C19.
Theranostics, 2021, 11(5):2364-2380
Theranostics, 2021, 11(5):2364-2380
J Virol, 2021, JVI.00190-21
S2380 Diosmetin Diosmetin (Luteolin 4-methyl ether)是在Spearmint, Oregano, 和许多其他植物中发现的生物类黄酮。
Mol Med Rep, 2020, 22(2):1335-1341
J Med Virol, 2019, 91(8):1440-1447
Int J Biol Sci, 2019, 15(11):2497-2508
S2526 Alizarin Alizarin是一种从茜草Rubia tinctorum L的根中提取的红色媒染剂。 Alizarin 能够强烈抑制 P450 同工型 CYP1A1CYP1A2CYP1B1,酶测定中的 IC50 分别为 6.2 μM、10.0 μM 和 2.7 μM 。 同时,也有文献报道Alizarin可增加 HepG2 细胞中 CYP1A1 酶活性,并作为 AHR 受体的激动剂。
Chem Res Toxicol, 2023, 36(8):1361-1373
BMC Med, 2022, 20(1):365
Cell Rep, 2020, 14;31(2):107518
S7456 Osilodrostat (LCI699) LCI699 (Osilodrostat) 是有效的11β-hydroxylase (CYP11B)抑制剂,11β-hydroxylase是催化皮质醇合成的最后一步。
Cells, 2022, 11(21)3344
Drug Metab Dispos, 2022, 50(2):114-127
J Inorg Biochem, 2022, 235:111934
S1195 Orteronel Orteronel(TAK-700)是一种有效的,高度选择性的,人17,20-lyase抑制剂,IC50为38 nM,比作用于其他CYPs(例如11-羟化酶和CYP3A4)选择性高1000倍以上。TAK-700 (Orteronel) 是一种雄性激素 androgen 生物合成抑制剂。Phase 3。
Toxicol Appl Pharmacol, 2023, 475:116638
Drug Metab Dispos, 2017, 45(6):635-645
Biochem Biophys Res Commun, 2016, 477(4):1005-10
S2401 Sodium Danshensu Sodium Danshensu是丹参素的单钠盐,是从Salvia miltiorrhiza Bge中分离的天然酚酸,是咖啡酸衍生物。
Molecules, 2023, 28(4)1551
Front Pharmacol, 2022, 13:946668
J Med Virol, 2019, 91(8):1440-1447
S3931 Ginsenoside Rd Ginsenoside Rd (Panaxoside Rd, Sanchinoside Rd), a minor ginseng saponin, has several pharmacological activities such as immunosuppressive activity, anti-inflammatory activity, immunological adjuvant, anti-cancer activity and wound-healing activity. Ginsenoside Rd inhibits TNFα-induced NF-κB transcriptional activity with an IC50 of 12.05±0.82 μM in HepG2 cells. Ginsenoside Rd inhibits expression of COX-2 and iNOS mRNA. Ginsenoside Rd also inhibits Ca2+ influx. Ginsenoside Rd inhibits CYP2D6, CYP1A2, CYP3A4, and CYP2C9, with IC50s of 58.0±4.5 μM, 78.4±5.3 μM, 81.7±2.6 μM, and 85.1±9.1 μM, respectively.
Drug Des Devel Ther, 2022, 16:2767-2782
J Ginseng Res, 2022, 46(5):700-709
J Ethnopharmacol, 2021, S0378-8741(21)00169-0
S3874 Curcumenol Curcumenol, a sesquiterpene isolated from Curcuma zedoaria, is known to possess a variety of health and medicinal values which includes neuroprotection, anti-inflammatory, anti-tumor and hepatoprotective activities. It inhibits NF-κB activation by suppressing the nuclear translocation of the NF-κB p65 subunit and blocking IκBα phosphorylation and degradation.
Front Pharmacol, 2022, 13:905966
J Bone Miner Res, 2021, 10.1002/jbmr.4328
Int J Mol Med, 2021, 48(4)192
S5266 Stiripentol Stiripentol (BCX2600) is a third-generation anti-epileptic drug that enhances GABAergic neurotransmission. It is an inhibitor of cytochrome P450.
Cell Metab, 2022, 34(1):90-105.e7
Front Pharmacol, 2021, 12:785586
S6868 Alflutinib (Furmonertinib) mesylate Alflutinib (Furmonertinib) mesylate是第三代 epidermal growth factor receptor (EGFR) 的抑制剂,可抑制EGFR敏感突变和T790M突变。Alflutinib (AST2818) 主要由CYP3A4代谢,也是有效的 CYP3A4 的诱导剂,EC50值为0.25 μM。
Int J Mol Sci, 2023, 24(18)13972
Int J Mol Sci, 2023, 24(18)13972
S3833 Amentoflavone Amentoflavone (Didemethyl Ginkgetin) is a biflavonoid originally isolated from Selaginella with antibacterial, antioxidant, antiviral, antidiabetic, and neuroprotective activities.
Front Plant Sci, 2021, 12:740923
Viruses, 2019, 11(5)E466
S5967 Berberine chloride hydrate Berberine (Natural Yellow 18) chloride hydrate 是属于异喹啉生物碱的季铵盐。Berberine 可激活 caspase 3caspase 8poly ADP-ribose polymerase (PARP) 的切割和 cytochrome c 的释放。Berberine chloride 可降低 c-IAP1Bcl-2Bcl-XL 的表达。Berberine chloride 通过 JNKp38 MAPK 的持续磷酸化以及 ROS的生成来诱导凋亡。Berberine chloride 是一种 topoisomerase III 的双重抑制剂。Berberine chloride 也是一种潜在的自噬调节剂。
Front Biosci (Landmark Ed), 2022, 27(8):242
Front Pharmacol, 2021, 12:632201
S3673 Sulfaphenazole Sulfaphenazole (Depocid, Depotsulfonamide, Plisulfan, Raziosulfa) is an inhibitor of CYP2C9 with Ki value of 0.3 μM and demonstrates at least 100-fold selectivity over other CYP450 isoforms (Ki values of 63 and 29 μM for CYP2C8 and CYP2C18, respectively, and no activity at CYP1A1, CYP1A2, CYP3A4, CYP2C19).
UNIVERSITY OF APPLIED SCIENCES, 2023,
Chem Biol Interact, 2022, 353:109801
Chem Biol Interact, 2022, 365:110070
S3917 Tetrahydrocurcumin Tetrahydrocurcumin (Tetrahydrodiferuloylmethane, Tetrahydro Curcumin), a major metabolite of curcumin, possesses strong antioxidant and cardioprotective properties.
J Gerontol A Biol Sci Med Sci, 2022, 77-8:1485-1493
Invest Ophthalmol Vis Sci, 2022, 63(6):26
S3660 Uniconazole (S 3307D) Uniconazole (S 3307D, XE 1019D) is a well known inhibitor of cytochrome P450 monooxygenase that prevents the biosynthesis of trans-zeatin. Uniconazole targets CYP735As with Ki of 22 μM.
Nat Microbiol, 2022, 10.1038/s41564-022-01072-5
Nat Biotechnol, 2021, 10.1038/s41587-021-00860-4
S2329 Naringin Naringin (Naringoside) 是一种黄酮苷,是葡萄柚中的主要的类黄酮,具有柚子汁的苦味。具有抗氧化,降血脂,抗肿瘤活性,并且对cytochrome P450有抑制作用。
Am J Transl Res, 2021, 13(6):6330-6341
Int J Mol Sci, 2020, 21(14):5025
S3273 Hypericin Hypericin (Hyp, HY) 是一种在 common St. John's Wort (Hypericum species) 中发现的天然物质,具有抗抑郁、抗肿瘤和抗病毒 (人类免疫缺陷病毒HIV和丙型肝炎病毒HCV) 活性。Hypericin 对 MAO (monoaminoxidase)PKC (protein kinase C)dopamine-beta-hydroxylasereverse transcriptasetelomeraseCYP (cytochrome P450)
Eur J Pharmacol, 2021, 900:174071
S5416 Metyrapone Metyrapone (NSC-25265, SU-4885) is an inhibitor of the enzyme steroid 11-beta-monooxygenase (CYP11B1) that inhibits adrenal steroid synthesis.
Cells, 2022, 11(21)3344
S6790 Ellipticine hydrochloride Ellipticine Hydrochloride (NSC 71795, PZE)是一种有效的 DNA topoisomerase II 的抑制剂,并通过其与 cytochromes P450 (CYP)peroxidases 的氧化作用介导形成共价DNA加合物。Ellipticine Hydrochloride 是从澳大利亚的夹竹桃科常绿乔木中分离出来的具有抗肿瘤活性的天然产物。
Viruses, 2022, 15(1)105
S3766 Tanshinone IIA sulfonate sodium Sodium tanshinone IIA sulfonate (STS) is a water-soluble derivative of tanshinone IIA isolated as the main pharmacologically active natural compound from a traditional Chinese herbal medicine, the dried root of Salvia miltiorrhiza Bunge known as Danshen. Sodium tanshinone IIA sulfonate (STS) is a potent negative allosteric modulator of the human purinergic receptor P2X7. Sodium tanshinone IIA sulfonate (STS) inhibits the activity of CYP3A4 and store-operated Ca2+ entry (SOCE) through store-operated Ca2+ channels (SOCC) via downregulating the expression of transient receptor potential canonical proteins (TRPC).
J Inflamm Res, 2022, 15:6293-6306
S4221 Benzbromarone Benzbromarone(Desuric) 是CYP2C9抑制剂,与CYP2C9 结合,Ki为19.3 nM。
Hum Mol Genet, 2020, ddaa244
S2344 Piperine Piperine (1-Piperoylpiperidine) 是一种生物碱,是造成黑胡椒和长胡椒辛辣的原因,也用于一些传统医学领域,且作为杀虫剂。
Int J Mol Med, 2015, 36(5):1369-76
S2496 Ozagrel Ozagrel (OKY-046)是一种有效的,选择性的血栓素A2合成酶抑制剂,IC50为4 nM。
S1739 Thiabendazole Thiabendazole 抑制线粒体蠕虫特异性酶,延胡索酸还原酶,具有驱虫药的性能。是一种有效的CYP1A2的抑制剂。
S2067 Ozagrel HCl Ozagrel HCl (OKY-046)是选择性血栓素A2合成酶抑制剂,其在兔子血小板中IC50为11 nM, 用作改善手术后脑血管收缩,以及伴随的脑梗塞。
S4155 Chlorzoxazone Chlorzoxazone(Chlorzoxazon,Paraflex)是一种肌肉松弛的药物,作为人体肝脏细胞色素P-450IIE1的探针。
S5169 2,6-Dihydroxyanthraquinone 2,6-Dihydroxyanthraquinone (Anthraflavic acid, Anthraflavin) is a potent and specific inhibitor of cytochrome P-448 activity.
S0721 Ticlopidine Ticlopidine (Yuclid, Ticlopidinum, Ticlopidina,PCR 5332) 是一种 adenosine diphosphate (ADP) 诱导的 platelet aggregation 的口服活性抑制剂。Ticlopidine 也是 CYP2B6 的抑制剂,Ki值为0.2 μM。
S0922 Salvianolic acid C Salvianolic acid C是一种非竞争性的细胞色素P4502C8 (Cytochrome P4502C8, CYP2C8)抑制剂和细胞色素P45022J2(Cytochrome P45022J2, CYP2J2)的中度混合抑制剂。
A5216 Cytochrome P450 2D6 Rabbit Recombinant mAb
S2921 PF-4981517 PF-4981517 (CYP3cide, PF-04981517) 是一种有效的,选择性的CYP3A4(P450)抑制剂,IC50为0.03 μM,比作用于CYP3A5和CYP3A7选择性高500倍以上。
S3291 Myristicin Myristicin (Myristicine) 是一种在 Myristica fragrans 的种子 Nutmeg 中的萜烯样活性成分,是 monamine oxidase (MAO) 的弱抑制剂和 CYP1A2 的机理抑制剂。
S5252 Ozagrel sodium Ozagrel sodium (KCT-0809, Cataclot, Xanbo) is a thromboxane A2 synthase (CYP5) inhibitor with neuroprotective properties.
E1650New Opevesostat (ODM208) Opevesostat (ODM208) 是一流的选择性非甾体口服 CYP11A1 抑制剂。 ODM208 在体外肾上腺皮质癌细胞模型、成年未去势雄性小鼠和狗以及 CRPC 患者中表现出快速、完全、持久和可逆的类固醇激素生物合成抑制作用。
A5239 Alas1 Rabbit Recombinant mAb
S0541 Dazoxiben hydrochloride Dazoxiben hydrochloride (HCl) 是一种 thromboxane (TX) synthase.的有效,选择性和口服活性抑制剂。Dazoxiben 可抑制人全血中 TXB2 的产生,其IC50值为0.3 μM,并可平行地增强 PGE2 的产生。
S9250 Isosilybin Isosilybin (Silymarin, Isosilybinin, Q-100795)是一种在水飞蓟(S. marianum)果实提取物中发现的黄烷醇,具有抗氧化和抗癌活性。Isosilybin 抑制 CYP3A4 诱导,IC50为74 μM。
S6606 CDD3505 CDD3505可通过诱导肝脏细胞色素P450IIIA活性,提高高密度脂蛋白胆固醇(HDL)水平。
S9257 Acetylshikonin Acetylshikonin is a biologically active compound with anti-cancer and anti-inflammatory activity, which is isolated from the roots of Lithospermum erythrorhizoma. It is a novel general P450 inhibitor with IC50 values of 1.4-4.0 μM for all tested P450s.
E0214New Pachymic acid Pachymic acid(3-O-Acetyltumulosic acid)抑制CYP2C9的活性,IC50为21.25 µM。
S4938 Cedrol Cedrol是一种天然存在的倍半萜烯醇,是有效的、竞争性的抑制剂,抑制CYP2B6介导的安非他酮羟化酶(bupropion hydroxylase),Ki值为0.9 μM。它还能抑制CYP3A4介导的咪达唑仑羟基化,Ki为3.4 μM。对CYP2C8, CYP2C9和CYP2C19的活性仅有微弱的抑制作用。
S2389 Naringin Dihydrochalcone Naringin Dihydrochalcone 是一种新型甜味剂,是来自柚皮苷的一种人工甜味剂。也是一种CYP enzymes的抑制剂。
S4741 Danshensu Danshensu (Salvianic acid A),是一种传统中药中的中草药,具有潜在的抗肿瘤和抗血管生成的效果。Danshensu 可抑制 CYP2E1CYP2C9,对应的IC50值分别为36.63 μm和 75.76 μm。
S2271 Berberine chloride Berberine chloride是异喹啉类生物碱的季铵盐。Berberine chloride 可激活 caspase 3caspase 8,分裂 poly ADP-ribose polymerase (PARP) 和释放 cytochrome c。Berberine chloride 可降低 c-IAP1Bcl-2Bcl-XL 的表达。Berberine chloride 可通过 JNKp38 MAPK 的持续磷酸化以及产生 ROS 来诱导凋亡。Berberine chloride 是一个 topoisomerase III 的双效抑制剂。Berberine chloride 也是一个潜在的自噬调节剂。
Adv Healthc Mater, 2023, e2300591.
Transl Oncol, 2023, 35:101712
J Biomol Struct Dyn, 2022, 1-11
A5282 Aromatase Rabbit Recombinant mAb
S9299 Ginsenoside F1 Ginsenoside F1 是人参的药物成分,已知具有抗衰老、抗氧化、抗癌和角质形成细胞的保护作用。Ginsenoside F1 对 CYP3A4 活性具有竞争性抑制作用,Ki值为67.8 ± 16.2 μM。Ginsenoside F1 对 CYP2D6 的抑制作用较弱。
S4963 Purpurin Purpurin (1,2,4-Trihydroxyanthraquinone, Hydroxylizaric acid, Verantin)是从茜草根和其他茜草科植物家族中分离出的天然色素。它具有抗血管生成、抗菌、抗氧化活性。Purpurin 可有效地抑制CYP1A1、CYP1A2 和 CYP1B1。
E0531 TMS TMS ((E)-2,3',4,5'-tetramethoxystilbene)是一种选择性和竞争性的人细胞色素P450s B1 (human cytochrome P450s B1, CYP1B1)抑制剂,IC50为6 nM。
S3777 Gentiopicroside Gentiopicroside (GE, Gentiopicrin), a naturally occurring iridoid glycoside, inhibits CYP2A6 and CYP2E1 with IC50 values of 21.8μg/ml and 594μg/ml, respectively in human liver microsomes, and dose not inhibit CYP2C9, CYP2D6, CYP1A2 or CYP3A4 activities.
S0110 APD597 APD-597 (JNJ-38431055) 是一种有效的、选择性的 G protein-coupled receptor 119 (GPR119) 的激动剂,对hGPR119的EC50值为46 nM,也是 Cytochrome P450 2C9 (CYP2C9) 的抑制剂,IC50值为5.8 μM。APD-597 (JNJ-38431055) 被开发用于治疗2型糖尿病(T2D)。
S5969 Dicloxacillin Sodium hydrate Dicloxacillin Sodium hydrate (DLX, Dycill, Dynapen, Pathocil) 是一种青霉素类的窄谱β-内酰胺抗生素,可在临床上水平上诱导药物代谢有关的 CYP enzymes 水平。
S4831 Piperonyl butoxide Piperonyl butoxide (PBO, Butacide, Ethanol butoxide, Pyrenone 606,ENT-14250)是一种人造的农药增效剂,与杀虫剂一起作用能够增强其有效性。
E2912New MEHP MEHP (Phthalic acid mono-2-ethylexyl ester) 是一种 CYP2C9 的竞争性抑制剂,IC50 为 6.37 μM。
S0175 DMU2105 DMU2105 是一种有效且特异的 CYP1B1 抑制剂,其IC50值为10 nM。
S0176 DMU2139 DMU2139 是一种有效且特异的 CYP1B1 抑制剂,其IC50值为9 nM。
S0418 Ezutromid Ezutromid (SMT C1100,BMN 195,VOX-C1100)是一种首创的口服活性苯并恶唑肌营养相关蛋白(utrophin)调节剂,EC50为0.91 μM,可用于杜氏营养不良症(Duchenne muscular dystrophy, DMD),还可抑制人肝微粒体(human liver microsomes, HLM)中CYP1A2的酶活性,IC50为5.4 μM。
S3719 Topiroxostat Topiroxostat is a xanthine oxidoreductase (XOR) inhibitor and used for treatment of gout and hyperuricemia. Topiroxostat exhibits weak CYP3A4-inhibitory activity (18.6%). Topiroxostat has the potential for hyperuricemia treatment.
S6886 1-Aminobenzotriazole 1-Aminobenzotriazole (ABT, 3-Aminobenzotriazole, 1-Benzotriazolylamine, NSC 114498, NSC 656987) 是一种非选择性且不可逆的 cytochrome P450 (CYP) enzymes 的抑制剂。1-Aminobenzotriazole 还是 N-acetyltransferase (NAT) 的底物和抑制剂。
S9442 Bergaptol Bergaptol (5-Hydroxypsoralen, 5-Hydroxyfuranocoumarin)是在柠檬、佛手柑等柑橘精油中发现的天然呋喃香豆素。Bergaptol 是有效的 CYP3A4 酶脱苄基活性抑制剂,IC50值为24.92 μM。
Molecules, 2024, 29(3)713
S5380 7-Hydroxyflavone 7-Hydroxyflavone is a potent inhibitor of CYP1A1 with a Ki value of 0.015 μM and exhibits 6-fold greater selectivity for CYP1A1 over CYP1A2. It also has excellent antioxidant properties and great potential to be applied as medicines.
S5529 Galangin Galangin (3,5,7-trihydroxyflavone; Norizalpinin), a naturally occuring flavonoid found in herbs, is a well-known antioxidant and also an inhibitor of CYP1A1 activity and an agonist/antagonist of the aryl hydrocarbon receptor.
S4784 Phloracetophenone Phloracetophenone, or 2,4,6-trihydroxyacetophenone (THA), the aglycone component of phloracetophenone glucoside, is a naturally occurring compound obtained from the rhizome of Curcuma comosa (Family Zingiberaceae).
S9241 Polygalaxanthone III Polygalaxanthone III 是一种天然产物,具有镇静,减轻感冒,消除痰液和消肿的功效。Polygalaxanthone III 抑制 CYP2E1 催化的氯唑沙宗6-羟基化反应,IC50值为50.56 μM。
S6594 Liarozole dihydrochloride Liarozole Dihydrochloride 是 P450 的温和抑制剂,对 CYP26 和大鼠 CYP17 的 IC50 分别为 2.2–6.0 μM 和 260 nM。
S9163 Rhapontigenin Rhapontigenin (Protigenin), produced from rhapontin isolated from a methanol extract of Rheum undulatum roots by enzymatic transformation, is a selective inactivator of cytochrome P450 1A1 (IC50 = 400 nM).
S0230 NVP-VID-400 NVP-VID-400 (SDZ285428) 是 CYP51 的抑制剂。NVP-VID-400 (SDZ285428) 抑制 T. cruziT. brucei 的I/E2a(5 min) 值均 <1 而 I/E2(60 min) 值分别为9和35。
S3227 5,7-Dimethoxyflavone 5,7-Dimethoxyflavone (5,7-DMF) 是一种 cytochrome P450 (CYP) 3As 的抑制剂,可显著地降低肝脏中CYP3A11和CYP3A25的表达。5,7-Dimethoxyflavone (5,7-DMF) 也是一种有效的 Breast Cancer Resistance Protein (BCRP, ABCG2) 的抑制剂。5,7-Dimethoxyflavone (5,7-DMF) 是Kaempferia parviflora的主要成分之一,具有抗肥胖、抗炎和抗肿瘤作用。
S6437 Oxolamine Citrate Oxolamine (SKF-9976, AF-438) citrate 是一种止咳药,是 CYP2B1/2 的抑制剂。Oxolamine citrate 也表现出抗炎作用。
S1185 Ritonavir Ritonavir是Cytochrome P450 3AHIV蛋白酶抑制剂,用于治疗HIV感染和AIDS。抑制Cytochrome P450 2D6, P-Glycoprotein,诱导Cytochrome P450 2C19, Cytochrome P450 1A2, Cytochrome P450 2C9, Cytochrome P450 2B6UDP Glucuronosyltransferases。Ritonavir 可诱导凋亡。
Cancer Drug Resist, 2024, 7:3
Int. J. Mol. Sci, 2023, 10.3390/ijms24076062
Int J Mol Sci, 2023, 24(7)6062
S2476 Itraconazole Itraconazole是一种三唑类抗真菌药物,是CYP3A4的有效抑制剂,IC50为6.1 nM。Itraconazole 是一个有效的Hedgehog (Hh)信号通路的拮抗剂。Itraconazole 可通过诱导自噬来抑制恶性胶质瘤的生长。
Front Cell Infect Microbiol, 2023, 13:1128000
Front Cell Infect Microbiol, 2022, 12:864912
Front Cell Infect Microbiol, 2022, 12:1074903
S1123 Abiraterone Abiraterone是一种有效CYP17抑制剂,无细胞试验中IC50为2 nM。Abiraterone (CB-7598) 是一种雄性激素 androgen 生物合成抑制剂。
Cancer Res, 2023, 83(8):1361-1380
Cancer Cell, 2021, S1535-6108(21)00659-0
Cancers (Basel), 2021, 13(16)3959
S2246 Abiraterone Acetate Abiraterone Acetate是Abiraterone的醋酸盐形式,是一种甾体类细胞色素CYP17抑制剂,无细胞试验中IC50为72 nM。Abiraterone acetateis 是一种口服的雄性激素 androgen 生物合成抑制剂。
Cancer Res, 2023, 83(2):219-238
J Immunother Cancer, 2023, 11(5)e006581
Pharmacol Res, 2023, 189:106692
S2262 Apigenin Apigenin是一种有效的CYP2C9抑制剂,Ki为2 μM.。
Transl Oncol, 2023, 35:101712
Molecules, 2023, 28(13)4947
Pharmacol Res, 2022, 185:106489
S2268 Baicalein Baicalein是CYP2C9和脯氨酰肽链内切酶抑制剂。
SLAS Discov, 2024, S2472-5552(24)00007-8
Redox Rep, 2023, 28(1):2152607
Microbiol Spectr, 2023, 11(3):e0470222
S1257 Posaconazole Posaconazole是CYP3A4的抑制剂,但不抑制其他CYP酶的活性;同时是sterol C14ɑ demethylase的抑制剂,IC50为0.25 μM。其平均的消除半衰期为15-35小时。
Front Cell Infect Microbiol, 2022, 12:1074903
Front Cell Infect Microbiol, 2022, 12:864912
Int J Mol Sci, 2022, 23(22)13809
S1331 Fluconazole Fluconazole是一种羊毛甾醇14 alpha去甲基化酶 抑制剂,抑制了麦角固醇的形成,用于治疗和预防浅表性和全身性真菌感染。
Front Cell Infect Microbiol, 2024, 14:1296151
Nat Commun, 2022, 13(1):1658
Nat Commun, 2022, 13(1):4295
S1353 Ketoconazole Ketoconazole能抑制cyclosporine oxidase(环孢素氧化酶)testosterone 6 beta-hydroxylase(睾丸素6β-羟化酶)IC50分别为0.19 mM和0.22 mM。Ketoconazole 是一种雄性激素 androgen 生物合成抑制剂。
J Med Virol, 2023, 95(6):e28856
Cell Death Dis, 2023, 14(1):64
Cell Death Dis, 2023, 14(8):488
S4202 Verapamil HCl Verapamil HCl是L-型钙通道抑制剂,是第四类抗心律失常的药剂。Verapamil 可抑制 permeability-glycoprotein (P-gp)CYP3A4
Cancers (Basel), 2023, 15(15)3774
EMBO Mol Med, 2022, 14(2):e14903
Cell Rep, 2022, 38(10):110468
S2187 Avasimibe Avasimibe 抑制ACATIC50为3.3 μM,也抑制人P450同工酶CYP2C9, CYP1A2和CYP2C19,IC50分别为2.9 μM, 13.9 μM和26.5 μM,
PLoS Pathog, 2023, 19(5):e1011323
Hepatol Int, 2023, 10.1007/s12072-023-10490-4
Front Pharmacol, 2022, 13:795934
S1794 Fenofibrate Fenofibrate是一种Fibrate类化合物,是纤维酸衍生物。Fenofibrate 是 PPARα 的选择性激动剂,EC50为30μM。Fenofibrate 可结合并抑制 cytochrome P450 epoxygenase (CYP)2C ,对于CYP2C19、CYP2B6和CYP2C9的IC50分别为0.2 μM、0.7 μM和9.7 μM。Fenofibrate 可诱导自噬。
Cancer Lett, 2023, 10.1016/j.canlet.2023.216427
Cell Metab, 2022, 34(2):299-316.e6
Cancers (Basel), 2022, 14(2)282
S2900 Cobicistat Cobicistat是一种有效的CYP3A选择性抑制剂,IC50为30 - 285 nM。
J Pers Med, 2022, 12(2)258
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Hum Cell, 2021, 34(6):1911-1918
S2046 Pioglitazone HCl Pioglitazone HCl (AD-4833, U-72107E) 是一种 cytochrome P450 (CYP)2C8CYP3A4 酶的抑制剂。Pioglitazone HCl 抑制CYP2C8、CYP3A4和CYP2C9的Ki值分别为1.7 μM、11.8 μM和32.1 μM。Pioglitazone HCl 也是一种选择性的 peroxisome proliferator-activated receptor-gamma (PPARγ) 激动剂,对人PPARγ和小鼠PPARγ的EC50值分别为0.93 μM和0.99 μM。Pioglitazone HCl 可抑制线粒体内铁的摄取、脂质过氧化和随后的铁死亡。
Commun Biol, 2022, 5(1):231
J Genet Genomics, 2022, S1673-8527(22)00133-3
J Cell Mol Med, 2022, 10.1111/jcmm.17154
S2394 Naringenin Naringenin (NSC 34875, S-Dihydrogenistein, NSC 11855, Salipurol)是来自于食用植物的一种天然的主要黄酮类化合物,有益人体健康,具有生物活性,是一种抗氧化剂,自由基清除剂,抗炎,碳水化合物代谢启动子及免疫系统的调制剂。
J Transl Med, 2024, 22(1):208
Molecules, 2023, 28(13)4947
Biomed Res Int, 2022, 2022:8080679
S4662 Atazanavir Atazanavir (Latazanavir, Zrivada, Reyataz, BMS-232632) 是一种氮杂肽及HIV-蛋白酶抑制剂,常与其他抗HIV药物结合,用于治疗HIV感染以及获得性免疫缺乏综合征。Atazanavir 是 cytochrome P450 isozyme 3A (CYP3A4) 的底物和抑制剂,也是 P-glycoprotein 的抑制剂和诱导剂。
Int J Mol Sci, 2022, 23(23)15380
Chemistry, 2022, e202202798.
Sci Rep, 2021, 11(1):19443
S1952 Methoxsalen Methoxsalen (Xanthotoxin, NCI-C55903) 是在一些植物中发现的天然存在的呋喃香豆素化合物,包括补骨脂,用于治疗牛皮癣,湿疹,白癜风及一些暴露在阳光下的皮肤淋巴瘤。是CYP2A5/6抑制剂。
J Pers Med, 2022, 12(2)258
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Hum Cell, 2021, 34(6):1911-1918
S2803 Galeterone Galeterone (TOK-001)是一种选择性CYP17抑制剂,也是androgen receptor (AR)(雄激素受体)拮抗剂,IC50分别为300 nM和384 nM,也有效抑制人类前列腺肿瘤生长。Phase 2。
ChemMedChem, 2022, e202200043
Cancer Chemother Pharmacol, 2020, 10.1007/s00280-020-04195-w
Steroids, 2020, 153:108534
S2555 Clarithromycin Clarithromycin (A-56268) 是一种大环内酯类抗生素,是CYP3A4抑制剂,用于治疗许多细菌感染。
Microorganisms, 2022, 10(7)1421
Cell Biol Toxicol, 2021, 10.1007/s10565-021-09646-5
J Ovarian Res, 2019, 12(1):107
S5658 Omeprazole Sodium Omeprazole Sodium is the sodium salt form of omeprazole, which is a proton pump inhibitor and suppresses gastric acid secretion. Omeprazole Sodium is a metabolism-dependent inhibitor (MDI) of CYP2C19.
Theranostics, 2021, 11(5):2364-2380
Theranostics, 2021, 11(5):2364-2380
J Virol, 2021, JVI.00190-21
S2380 Diosmetin Diosmetin (Luteolin 4-methyl ether)是在Spearmint, Oregano, 和许多其他植物中发现的生物类黄酮。
Mol Med Rep, 2020, 22(2):1335-1341
J Med Virol, 2019, 91(8):1440-1447
Int J Biol Sci, 2019, 15(11):2497-2508
S2526 Alizarin Alizarin是一种从茜草Rubia tinctorum L的根中提取的红色媒染剂。 Alizarin 能够强烈抑制 P450 同工型 CYP1A1CYP1A2CYP1B1,酶测定中的 IC50 分别为 6.2 μM、10.0 μM 和 2.7 μM 。 同时,也有文献报道Alizarin可增加 HepG2 细胞中 CYP1A1 酶活性,并作为 AHR 受体的激动剂。
Chem Res Toxicol, 2023, 36(8):1361-1373
BMC Med, 2022, 20(1):365
Cell Rep, 2020, 14;31(2):107518
S7456 Osilodrostat (LCI699) LCI699 (Osilodrostat) 是有效的11β-hydroxylase (CYP11B)抑制剂,11β-hydroxylase是催化皮质醇合成的最后一步。
Cells, 2022, 11(21)3344
Drug Metab Dispos, 2022, 50(2):114-127
J Inorg Biochem, 2022, 235:111934
S1195 Orteronel Orteronel(TAK-700)是一种有效的,高度选择性的,人17,20-lyase抑制剂,IC50为38 nM,比作用于其他CYPs(例如11-羟化酶和CYP3A4)选择性高1000倍以上。TAK-700 (Orteronel) 是一种雄性激素 androgen 生物合成抑制剂。Phase 3。
Toxicol Appl Pharmacol, 2023, 475:116638
Drug Metab Dispos, 2017, 45(6):635-645
Biochem Biophys Res Commun, 2016, 477(4):1005-10
S2401 Sodium Danshensu Sodium Danshensu是丹参素的单钠盐,是从Salvia miltiorrhiza Bge中分离的天然酚酸,是咖啡酸衍生物。
Molecules, 2023, 28(4)1551
Front Pharmacol, 2022, 13:946668
J Med Virol, 2019, 91(8):1440-1447
S3931 Ginsenoside Rd Ginsenoside Rd (Panaxoside Rd, Sanchinoside Rd), a minor ginseng saponin, has several pharmacological activities such as immunosuppressive activity, anti-inflammatory activity, immunological adjuvant, anti-cancer activity and wound-healing activity. Ginsenoside Rd inhibits TNFα-induced NF-κB transcriptional activity with an IC50 of 12.05±0.82 μM in HepG2 cells. Ginsenoside Rd inhibits expression of COX-2 and iNOS mRNA. Ginsenoside Rd also inhibits Ca2+ influx. Ginsenoside Rd inhibits CYP2D6, CYP1A2, CYP3A4, and CYP2C9, with IC50s of 58.0±4.5 μM, 78.4±5.3 μM, 81.7±2.6 μM, and 85.1±9.1 μM, respectively.
Drug Des Devel Ther, 2022, 16:2767-2782
J Ginseng Res, 2022, 46(5):700-709
J Ethnopharmacol, 2021, S0378-8741(21)00169-0
S3874 Curcumenol Curcumenol, a sesquiterpene isolated from Curcuma zedoaria, is known to possess a variety of health and medicinal values which includes neuroprotection, anti-inflammatory, anti-tumor and hepatoprotective activities. It inhibits NF-κB activation by suppressing the nuclear translocation of the NF-κB p65 subunit and blocking IκBα phosphorylation and degradation.
Front Pharmacol, 2022, 13:905966
J Bone Miner Res, 2021, 10.1002/jbmr.4328
Int J Mol Med, 2021, 48(4)192
S5266 Stiripentol Stiripentol (BCX2600) is a third-generation anti-epileptic drug that enhances GABAergic neurotransmission. It is an inhibitor of cytochrome P450.
Cell Metab, 2022, 34(1):90-105.e7
Front Pharmacol, 2021, 12:785586
S3673 Sulfaphenazole Sulfaphenazole (Depocid, Depotsulfonamide, Plisulfan, Raziosulfa) is an inhibitor of CYP2C9 with Ki value of 0.3 μM and demonstrates at least 100-fold selectivity over other CYP450 isoforms (Ki values of 63 and 29 μM for CYP2C8 and CYP2C18, respectively, and no activity at CYP1A1, CYP1A2, CYP3A4, CYP2C19).
UNIVERSITY OF APPLIED SCIENCES, 2023,
Chem Biol Interact, 2022, 353:109801
Chem Biol Interact, 2022, 365:110070
S3917 Tetrahydrocurcumin Tetrahydrocurcumin (Tetrahydrodiferuloylmethane, Tetrahydro Curcumin), a major metabolite of curcumin, possesses strong antioxidant and cardioprotective properties.
J Gerontol A Biol Sci Med Sci, 2022, 77-8:1485-1493
Invest Ophthalmol Vis Sci, 2022, 63(6):26
S3660 Uniconazole (S 3307D) Uniconazole (S 3307D, XE 1019D) is a well known inhibitor of cytochrome P450 monooxygenase that prevents the biosynthesis of trans-zeatin. Uniconazole targets CYP735As with Ki of 22 μM.
Nat Microbiol, 2022, 10.1038/s41564-022-01072-5
Nat Biotechnol, 2021, 10.1038/s41587-021-00860-4
S2329 Naringin Naringin (Naringoside) 是一种黄酮苷,是葡萄柚中的主要的类黄酮,具有柚子汁的苦味。具有抗氧化,降血脂,抗肿瘤活性,并且对cytochrome P450有抑制作用。
Am J Transl Res, 2021, 13(6):6330-6341
Int J Mol Sci, 2020, 21(14):5025
S3273 Hypericin Hypericin (Hyp, HY) 是一种在 common St. John's Wort (Hypericum species) 中发现的天然物质,具有抗抑郁、抗肿瘤和抗病毒 (人类免疫缺陷病毒HIV和丙型肝炎病毒HCV) 活性。Hypericin 对 MAO (monoaminoxidase)PKC (protein kinase C)dopamine-beta-hydroxylasereverse transcriptasetelomeraseCYP (cytochrome P450)
Eur J Pharmacol, 2021, 900:174071
S5416 Metyrapone Metyrapone (NSC-25265, SU-4885) is an inhibitor of the enzyme steroid 11-beta-monooxygenase (CYP11B1) that inhibits adrenal steroid synthesis.
Cells, 2022, 11(21)3344
S3766 Tanshinone IIA sulfonate sodium Sodium tanshinone IIA sulfonate (STS) is a water-soluble derivative of tanshinone IIA isolated as the main pharmacologically active natural compound from a traditional Chinese herbal medicine, the dried root of Salvia miltiorrhiza Bunge known as Danshen. Sodium tanshinone IIA sulfonate (STS) is a potent negative allosteric modulator of the human purinergic receptor P2X7. Sodium tanshinone IIA sulfonate (STS) inhibits the activity of CYP3A4 and store-operated Ca2+ entry (SOCE) through store-operated Ca2+ channels (SOCC) via downregulating the expression of transient receptor potential canonical proteins (TRPC).
J Inflamm Res, 2022, 15:6293-6306
S4221 Benzbromarone Benzbromarone(Desuric) 是CYP2C9抑制剂,与CYP2C9 结合,Ki为19.3 nM。
Hum Mol Genet, 2020, ddaa244
S2344 Piperine Piperine (1-Piperoylpiperidine) 是一种生物碱,是造成黑胡椒和长胡椒辛辣的原因,也用于一些传统医学领域,且作为杀虫剂。
Int J Mol Med, 2015, 36(5):1369-76
S2496 Ozagrel Ozagrel (OKY-046)是一种有效的,选择性的血栓素A2合成酶抑制剂,IC50为4 nM。
S1739 Thiabendazole Thiabendazole 抑制线粒体蠕虫特异性酶,延胡索酸还原酶,具有驱虫药的性能。是一种有效的CYP1A2的抑制剂。
S2067 Ozagrel HCl Ozagrel HCl (OKY-046)是选择性血栓素A2合成酶抑制剂,其在兔子血小板中IC50为11 nM, 用作改善手术后脑血管收缩,以及伴随的脑梗塞。
S5169 2,6-Dihydroxyanthraquinone 2,6-Dihydroxyanthraquinone (Anthraflavic acid, Anthraflavin) is a potent and specific inhibitor of cytochrome P-448 activity.
S0721 Ticlopidine Ticlopidine (Yuclid, Ticlopidinum, Ticlopidina,PCR 5332) 是一种 adenosine diphosphate (ADP) 诱导的 platelet aggregation 的口服活性抑制剂。Ticlopidine 也是 CYP2B6 的抑制剂,Ki值为0.2 μM。
S0922 Salvianolic acid C Salvianolic acid C是一种非竞争性的细胞色素P4502C8 (Cytochrome P4502C8, CYP2C8)抑制剂和细胞色素P45022J2(Cytochrome P45022J2, CYP2J2)的中度混合抑制剂。
S2921 PF-4981517 PF-4981517 (CYP3cide, PF-04981517) 是一种有效的,选择性的CYP3A4(P450)抑制剂,IC50为0.03 μM,比作用于CYP3A5和CYP3A7选择性高500倍以上。
S3291 Myristicin Myristicin (Myristicine) 是一种在 Myristica fragrans 的种子 Nutmeg 中的萜烯样活性成分,是 monamine oxidase (MAO) 的弱抑制剂和 CYP1A2 的机理抑制剂。
S5252 Ozagrel sodium Ozagrel sodium (KCT-0809, Cataclot, Xanbo) is a thromboxane A2 synthase (CYP5) inhibitor with neuroprotective properties.
E1650New Opevesostat (ODM208) Opevesostat (ODM208) 是一流的选择性非甾体口服 CYP11A1 抑制剂。 ODM208 在体外肾上腺皮质癌细胞模型、成年未去势雄性小鼠和狗以及 CRPC 患者中表现出快速、完全、持久和可逆的类固醇激素生物合成抑制作用。
S0541 Dazoxiben hydrochloride Dazoxiben hydrochloride (HCl) 是一种 thromboxane (TX) synthase.的有效,选择性和口服活性抑制剂。Dazoxiben 可抑制人全血中 TXB2 的产生,其IC50值为0.3 μM,并可平行地增强 PGE2 的产生。
S9250 Isosilybin Isosilybin (Silymarin, Isosilybinin, Q-100795)是一种在水飞蓟(S. marianum)果实提取物中发现的黄烷醇,具有抗氧化和抗癌活性。Isosilybin 抑制 CYP3A4 诱导,IC50为74 μM。
S9257 Acetylshikonin Acetylshikonin is a biologically active compound with anti-cancer and anti-inflammatory activity, which is isolated from the roots of Lithospermum erythrorhizoma. It is a novel general P450 inhibitor with IC50 values of 1.4-4.0 μM for all tested P450s.
E0214New Pachymic acid Pachymic acid(3-O-Acetyltumulosic acid)抑制CYP2C9的活性,IC50为21.25 µM。
S4938 Cedrol Cedrol是一种天然存在的倍半萜烯醇,是有效的、竞争性的抑制剂,抑制CYP2B6介导的安非他酮羟化酶(bupropion hydroxylase),Ki值为0.9 μM。它还能抑制CYP3A4介导的咪达唑仑羟基化,Ki为3.4 μM。对CYP2C8, CYP2C9和CYP2C19的活性仅有微弱的抑制作用。
S2389 Naringin Dihydrochalcone Naringin Dihydrochalcone 是一种新型甜味剂,是来自柚皮苷的一种人工甜味剂。也是一种CYP enzymes的抑制剂。
S9299 Ginsenoside F1 Ginsenoside F1 是人参的药物成分,已知具有抗衰老、抗氧化、抗癌和角质形成细胞的保护作用。Ginsenoside F1 对 CYP3A4 活性具有竞争性抑制作用,Ki值为67.8 ± 16.2 μM。Ginsenoside F1 对 CYP2D6 的抑制作用较弱。
S4963 Purpurin Purpurin (1,2,4-Trihydroxyanthraquinone, Hydroxylizaric acid, Verantin)是从茜草根和其他茜草科植物家族中分离出的天然色素。它具有抗血管生成、抗菌、抗氧化活性。Purpurin 可有效地抑制CYP1A1、CYP1A2 和 CYP1B1。
E0531 TMS TMS ((E)-2,3',4,5'-tetramethoxystilbene)是一种选择性和竞争性的人细胞色素P450s B1 (human cytochrome P450s B1, CYP1B1)抑制剂,IC50为6 nM。
S3777 Gentiopicroside Gentiopicroside (GE, Gentiopicrin), a naturally occurring iridoid glycoside, inhibits CYP2A6 and CYP2E1 with IC50 values of 21.8μg/ml and 594μg/ml, respectively in human liver microsomes, and dose not inhibit CYP2C9, CYP2D6, CYP1A2 or CYP3A4 activities.
S0110 APD597 APD-597 (JNJ-38431055) 是一种有效的、选择性的 G protein-coupled receptor 119 (GPR119) 的激动剂,对hGPR119的EC50值为46 nM,也是 Cytochrome P450 2C9 (CYP2C9) 的抑制剂,IC50值为5.8 μM。APD-597 (JNJ-38431055) 被开发用于治疗2型糖尿病(T2D)。
S4831 Piperonyl butoxide Piperonyl butoxide (PBO, Butacide, Ethanol butoxide, Pyrenone 606,ENT-14250)是一种人造的农药增效剂,与杀虫剂一起作用能够增强其有效性。
E2912New MEHP MEHP (Phthalic acid mono-2-ethylexyl ester) 是一种 CYP2C9 的竞争性抑制剂,IC50 为 6.37 μM。
S0175 DMU2105 DMU2105 是一种有效且特异的 CYP1B1 抑制剂,其IC50值为10 nM。
S0176 DMU2139 DMU2139 是一种有效且特异的 CYP1B1 抑制剂,其IC50值为9 nM。
S0418 Ezutromid Ezutromid (SMT C1100,BMN 195,VOX-C1100)是一种首创的口服活性苯并恶唑肌营养相关蛋白(utrophin)调节剂,EC50为0.91 μM,可用于杜氏营养不良症(Duchenne muscular dystrophy, DMD),还可抑制人肝微粒体(human liver microsomes, HLM)中CYP1A2的酶活性,IC50为5.4 μM。
S3719 Topiroxostat Topiroxostat is a xanthine oxidoreductase (XOR) inhibitor and used for treatment of gout and hyperuricemia. Topiroxostat exhibits weak CYP3A4-inhibitory activity (18.6%). Topiroxostat has the potential for hyperuricemia treatment.
S6886 1-Aminobenzotriazole 1-Aminobenzotriazole (ABT, 3-Aminobenzotriazole, 1-Benzotriazolylamine, NSC 114498, NSC 656987) 是一种非选择性且不可逆的 cytochrome P450 (CYP) enzymes 的抑制剂。1-Aminobenzotriazole 还是 N-acetyltransferase (NAT) 的底物和抑制剂。
S9442 Bergaptol Bergaptol (5-Hydroxypsoralen, 5-Hydroxyfuranocoumarin)是在柠檬、佛手柑等柑橘精油中发现的天然呋喃香豆素。Bergaptol 是有效的 CYP3A4 酶脱苄基活性抑制剂,IC50值为24.92 μM。
Molecules, 2024, 29(3)713
S5380 7-Hydroxyflavone 7-Hydroxyflavone is a potent inhibitor of CYP1A1 with a Ki value of 0.015 μM and exhibits 6-fold greater selectivity for CYP1A1 over CYP1A2. It also has excellent antioxidant properties and great potential to be applied as medicines.
S5529 Galangin Galangin (3,5,7-trihydroxyflavone; Norizalpinin), a naturally occuring flavonoid found in herbs, is a well-known antioxidant and also an inhibitor of CYP1A1 activity and an agonist/antagonist of the aryl hydrocarbon receptor.
S9241 Polygalaxanthone III Polygalaxanthone III 是一种天然产物,具有镇静,减轻感冒,消除痰液和消肿的功效。Polygalaxanthone III 抑制 CYP2E1 催化的氯唑沙宗6-羟基化反应,IC50值为50.56 μM。
S6594 Liarozole dihydrochloride Liarozole Dihydrochloride 是 P450 的温和抑制剂,对 CYP26 和大鼠 CYP17 的 IC50 分别为 2.2–6.0 μM 和 260 nM。
S9163 Rhapontigenin Rhapontigenin (Protigenin), produced from rhapontin isolated from a methanol extract of Rheum undulatum roots by enzymatic transformation, is a selective inactivator of cytochrome P450 1A1 (IC50 = 400 nM).
S0230 NVP-VID-400 NVP-VID-400 (SDZ285428) 是 CYP51 的抑制剂。NVP-VID-400 (SDZ285428) 抑制 T. cruziT. brucei 的I/E2a(5 min) 值均 <1 而 I/E2(60 min) 值分别为9和35。
S3227 5,7-Dimethoxyflavone 5,7-Dimethoxyflavone (5,7-DMF) 是一种 cytochrome P450 (CYP) 3As 的抑制剂,可显著地降低肝脏中CYP3A11和CYP3A25的表达。5,7-Dimethoxyflavone (5,7-DMF) 也是一种有效的 Breast Cancer Resistance Protein (BCRP, ABCG2) 的抑制剂。5,7-Dimethoxyflavone (5,7-DMF) 是Kaempferia parviflora的主要成分之一,具有抗肥胖、抗炎和抗肿瘤作用。
S6437 Oxolamine Citrate Oxolamine (SKF-9976, AF-438) citrate 是一种止咳药,是 CYP2B1/2 的抑制剂。Oxolamine citrate 也表现出抗炎作用。
A5216 Cytochrome P450 2D6 Rabbit Recombinant mAb
A5239 Alas1 Rabbit Recombinant mAb
A5282 Aromatase Rabbit Recombinant mAb
S6868 Alflutinib (Furmonertinib) mesylate Alflutinib (Furmonertinib) mesylate是第三代 epidermal growth factor receptor (EGFR) 的抑制剂,可抑制EGFR敏感突变和T790M突变。Alflutinib (AST2818) 主要由CYP3A4代谢,也是有效的 CYP3A4 的诱导剂,EC50值为0.25 μM。
Int J Mol Sci, 2023, 24(18)13972
Int J Mol Sci, 2023, 24(18)13972
S5967 Berberine chloride hydrate Berberine (Natural Yellow 18) chloride hydrate 是属于异喹啉生物碱的季铵盐。Berberine 可激活 caspase 3caspase 8poly ADP-ribose polymerase (PARP) 的切割和 cytochrome c 的释放。Berberine chloride 可降低 c-IAP1Bcl-2Bcl-XL 的表达。Berberine chloride 通过 JNKp38 MAPK 的持续磷酸化以及 ROS的生成来诱导凋亡。Berberine chloride 是一种 topoisomerase III 的双重抑制剂。Berberine chloride 也是一种潜在的自噬调节剂。
Front Biosci (Landmark Ed), 2022, 27(8):242
Front Pharmacol, 2021, 12:632201
S2271 Berberine chloride Berberine chloride是异喹啉类生物碱的季铵盐。Berberine chloride 可激活 caspase 3caspase 8,分裂 poly ADP-ribose polymerase (PARP) 和释放 cytochrome c。Berberine chloride 可降低 c-IAP1Bcl-2Bcl-XL 的表达。Berberine chloride 可通过 JNKp38 MAPK 的持续磷酸化以及产生 ROS 来诱导凋亡。Berberine chloride 是一个 topoisomerase III 的双效抑制剂。Berberine chloride 也是一个潜在的自噬调节剂。
Adv Healthc Mater, 2023, e2300591.
Transl Oncol, 2023, 35:101712
J Biomol Struct Dyn, 2022, 1-11
S4784 Phloracetophenone Phloracetophenone, or 2,4,6-trihydroxyacetophenone (THA), the aglycone component of phloracetophenone glucoside, is a naturally occurring compound obtained from the rhizome of Curcuma comosa (Family Zingiberaceae).
S6606 CDD3505 CDD3505可通过诱导肝脏细胞色素P450IIIA活性,提高高密度脂蛋白胆固醇(HDL)水平。
S5969 Dicloxacillin Sodium hydrate Dicloxacillin Sodium hydrate (DLX, Dycill, Dynapen, Pathocil) 是一种青霉素类的窄谱β-内酰胺抗生素,可在临床上水平上诱导药物代谢有关的 CYP enzymes 水平。
E1650New Opevesostat (ODM208) Opevesostat (ODM208) 是一流的选择性非甾体口服 CYP11A1 抑制剂。 ODM208 在体外肾上腺皮质癌细胞模型、成年未去势雄性小鼠和狗以及 CRPC 患者中表现出快速、完全、持久和可逆的类固醇激素生物合成抑制作用。
E0214New Pachymic acid Pachymic acid(3-O-Acetyltumulosic acid)抑制CYP2C9的活性,IC50为21.25 µM。
E2912New MEHP MEHP (Phthalic acid mono-2-ethylexyl ester) 是一种 CYP2C9 的竞争性抑制剂,IC50 为 6.37 μM。

P450 (e.g. CYP17)抑制剂选择性比较

Tags: P450 (e.g. CYP17) inhibitor|P450 (e.g. CYP17) agonist|P450 (e.g. CYP17) activator|P450 (e.g. CYP17) inducer|P450 (e.g. CYP17) antagonist|P450 (e.g. CYP17) signaling pathway|P450 (e.g. CYP17) assay kit
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