PPAR

PPAR抑制剂选择性比较

PPAR信号通路图

PPAR信号通路图

PPAR产品

  • 所有产品(53)
  • PPAR抑制剂 (10)
  • PPAR激活剂 (12)
  • PPAR拮抗剂 (5)
  • PPAR激动剂 (22)
  • PPAR调节剂 (4)
目录号 产品名 产品描述 文献引用 实验数据
S2871 T0070907 T0070907是一种有效的,选择性PPARγ抑制剂,无细胞试验中IC50为1 nM,比作用于PPARα和PPARδ选择性高800倍以上。T0070907 在ME-180和SiHa细胞中可显著降低 DNA-PKcsRAD51 蛋白的表达水平。
Redox Biol, 2022, 50:102256
Biomed Pharmacother, 2022, 151:113109
Exp Neurol, 2022, 354:114100
S8046New GW7647 GW7647是一种有效的PPARα激动剂,对人PPARα、PPARγ和PPARδ的EC50分别为6 nM、1.1 μM和6.2 μM。
S7767 AZ6102 AZ6102是有效的TNKS1/2抑制剂,选择性比作用于其他PARP家族的激酶高100倍,其在DLD-1细胞中抑制Wnt信号通路(IC50为5 nM)。
Sci Adv, 2022, 8(19):eabh2332
Haematologica, 2021, 10.3324/haematol.2020.267096
Nat Commun, 2019, 10(1):4898
S2798 GW6471 GW 6471 是一种 PPARα 的有效拮抗剂,其IC50值为0.24 μM。
Cancer Discov, 2022, candisc.1181.2021
J Mol Endocrinol, 2022, JME-21-0239
Cell Rep, 2021, 37(6):109920
S7484 FH535 FH535是一种Wnt/β-catenin信号传导抑制剂,同时也是PPARγPPARδ的双重拮抗剂。
Cell Death Dis, 2022, 13(5):493
Sci Rep, 2022, 12(1):7
J Exp Clin Cancer Res, 2021, 40(1):230
S5824 Cinnamyl alcohol Cinnamyl alcohol是一种存在于肉桂中的天然产物。
S5113 Propyl gallate Propyl gallate (Gallic acid propyl esterZ, n-Propyl gallate) is an antioxidant used in foods especially animal fats and vegetable oils, also in a wide variety of cosmetics and beauty care products.
S4527 Fenofibric acid Fenofibric acid (NSC 281318, Trilipix, FNF acid)是一种降脂剂,降低低密度脂蛋白胆固醇和甘油三脂。
Int J Pharm, 2019, 570:118661
S9129 20(S)-Ginsenoside Rh1 20(S)-Ginsenoside Rh1 (Prosapogenin A2, Sanchinoside B2, Sanchinoside Rh1)是从红参中提取的主要生物活性化合物之一,在世界范围内,红参已越来越多地用于增强认知和身体健康。它具有抗发炎、抗氧化、免疫调节作用和对神经系统有积极作用的有效特性。20(S)-Ginsenoside Rh1 可抑制 PPAR-γTNF-αIL-6IL-1β 的表达。
S7867 Oleuropein Oleuropein 是一种从橄榄叶中分离出的抗氧化多酚。Oleuropein 具有抗氧化、抗炎和抗动脉粥样硬化的作用,并在体外抑制脂肪细胞的分化。Oleuropein 抑制 PPARγ 活性。Oleuropein 通过直接抑制PPARγ转录活性发挥抗脂肪形成作用。Oleuropein 还可抑制aromatase。Oleuropein 可诱导凋亡。Phase 2。
J Med Virol, 2019, 91(8):1440-1447
E0473New CUDA CUDA是一种有效的可溶性环氧化物水解酶(soluble epoxide hydrolase, sEH)抑制剂,对小鼠和人sEH的IC50s分别为11.1 nM和112 nM,也能选择性地增加过氧化物酶体增殖物激活受体(peroxisome proliferator-activated receptor alpha, PPAR alpha)的活性。
S8029 WY-14643 (Pirinixic Acid) WY-14643 (Pirinixic Acid, NSC 310038) 是一种有效的选择性 PPARα 激活剂,EC50 为 1.5 μM。
Haematologica, 2021, 10.3324/haematol.2021.279770
Free Radic Biol Med, 2021, 169:283-293
Aging (Albany NY), 2021, 13(8):11969-11987
S1729 Gemfibrozil Gemfibrozil (CI-719) 是一种降低血脂水平的化合物。
S1849 Daidzein Daidzein属于异黄酮类。
J Mol Neurosci, 2018, 64(2):211-223
S9189 Oroxin A Oroxin A (Baicalein 7-O-glucoside), an active component isolated from the herb Oroxylum indicum (L.) Kurz, activates PPARγ and inhibits α-glucosidase, exerting antioxidant activity.
S3290 Procyanidin B2 Procyanidin B2 (PCB2) 是一种存在于常见食品中的天然类黄酮,具有抗炎、抗氧化和抗癌活性。Procyanidin B2 可激活 PPARγ 并诱导小鼠巨噬细胞M2极化。Procyanidin B2 可显著抑制百草枯在大鼠模型中肺组织中 NLRP3 炎性小体的活化。
S9723 CDDO-Im CDDO-Im (CDDO-Imidazolide, RTA-403, TP-235) 是一种 nuclear factor erythroid 2–related factor 2 (Nrf2)peroxisome proliferator-activated receptor (PPAR) 的激活剂。CDDO-Im 可与PPARα和PPARγ结合,对应的Ki值分别以232 nM和344 nM。CDDO-Im 在体内抑制炎症反应和肿瘤生长。
S5121 Phytol Phytol (Trans-Phytol), a diterpene alcohol from chlorophyll widely used as a food additive and in medicinal fields, shows antinociceptive and antioxidant activities as well as anti-inflammatory and antiallergic effects. It is a specific activator of PPARα.
S3875 Alpinetin Alpinetin, a composition of Alpinia katsumadai Hayata, has been reported to have a number of biological properties, such as antibacterial, antitumor and other important therapeutic activities.
Nutrients, 2021, 13(10)3382
S5851 4'-Methoxychalcone 4'-Methoxychalcone存在于柑橘属植物中,是一种查耳酮衍生物,具有多种药理活性,如抗肿瘤和消炎活性。
S4708 Palmitoylethanolamide Palmitoylethanolamide (PEA, Palmidrol, N-palmitoylethanolamine) 是一种内源性的脂肪酸酰胺,能在体外选择性激活PPAR-α,EC50为3.1±0.4 μM。
Neurosci Insights, 2020, 15:2633105520975412
J Steroid Biochem Mol Biol, 2019, 10.1016/j.jsbmb.2018.07.005
S9177 Gypenoside XLIX Gypenoside XLIX, a naturally occurring gynosaponin, is a selective peroxisome proliferator-activated receptor (PPAR)-alpha activator.
S2915 GW9662 GW9662是一种选择性PPAR拮抗剂,作用于PPARγ,无细胞试验中IC50为3.3 nM,在细胞中作用于PPARγ比作用于PPARα和PPARδ的功能选择性强10到600倍。
Brain Behav Immun, 2022, S0889-1591(22)00025-3
Free Radic Biol Med, 2022, 186:1-16
Oxid Med Cell Longev, 2022, 2022:9226022
S8025 GSK3787 GSK3787是一种选择性的,不可逆PPARδ拮抗剂,pIC50为6.6,对hPPARα和hPPARγ没有亲和力。
Cancer Discov, 2022, candisc.1181.2021
J Mol Endocrinol, 2022, JME-21-0239
Cell Death Dis, 2021, 12(3):240
S0531 DG172 dihydrochloride DG-172 dihydrochloride是一种新型的PPARβ/δ选择性拮抗剂,IC50为27 nM。
Cell Signal, 2022, 93:110304
S0773 Mifobate Mifobate (SR-202)是一种有效的特异性PPARγ拮抗剂,可选择性地抑制噻唑烷二酮(TZD)诱导的PPARγ转录活性(IC50=140 μM)。
S5817 GSK0660 GSK0660是有效的PPARβ/δ拮抗剂,pIC50为6.8。在浓度高达近于10 μM时,对PPARα和PPARγ没有活性。
Nat Commun, 2019, 11;10(1):4621
S2505 Rosiglitazone (BRL-49653) maleate Rosiglitazone maleate (BRL 49653) 是一种噻唑烷二酮类抗高血糖药,是PPARγ的高亲和、选择性的激动剂,IC50为42 nM。Rosiglitazone maleate 也能调节 TRP channels并诱导自噬。Rosiglitazone 可预防铁死亡。
Cell Death Dis, 2021, 12(11):972
Antioxidants (Basel), 2021, 10(2)155
Front Cardiovasc Med, 2021, 8:698056
S2556 Rosiglitazone (BRL 49653) Rosiglitazone (BRL 49653) 是有效的降糖药,也是有效的噻唑烷二酮类胰岛素增敏剂,在大鼠,3T3-L1和人体脂肪细胞中IC50分别为12,4和9 nM。Rosiglitazone是PPAR-gamma的配体,对PPAR-alpha没有结合力。Rosiglitazone 可调控 TRP channels 并诱导自噬。Rosiglitazone可阻止铁死亡。
Redox Biol, 2022, 50:102256
Toxicology, 2022, 465:153048
Hum Cell, 2022, 10.1007/s13577-022-00671-y
S2590 Pioglitazone (AD-4833) Pioglitazone (AD-4833, U 72107)是一种选择性过氧化物酶体增殖物激活受体γ (PPARγ) 激动剂, 用于治疗糖尿病。是全长hPPARα的弱激活剂,对全长hPPARδ没有作用。
Commun Biol, 2022, 5(1):231
Exp Neurol, 2022, 354:114100
J Genet Genomics, 2022, S1673-8527(22)00133-3
S8020 GW0742 GW0742是一种有效的,选择性PPARβ/δ激动剂,IC50为1 nM,比作用于hPPARα和hPPARγ选择性高1000倍。
Life Sci, 2021, 279:119696
Cells, 2019, 8(12)
Int J Med Sci, 2019, 16(12):1593-1603
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
Cell Immunol, 2022, 378:104556
S2665 Ciprofibrate Ciprofibrate (Win-35833)是一种过氧化物酶体增殖物激活受体激动剂。
Respir Physiol Neurobiol, 2020, 271:103290
S4159 Bezafibrate Bezafibrate (BM 15075) 是第一个临床测试的双重pan-peroxisome proliferator-activated receptors (PPAR)(过氧化物酶体增殖物激活受体)联合激动剂。
Nat Commun, 2021, 12(1):1929
PPAR Res, 2021, 2021:5589342
S4207 Clofibric Acid Clofibric acid 是PPARα激动剂,是一种降血脂剂。
S1794 Fenofibrate (NSC-281319) Fenofibrate (NSC-281319)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。
Cell Metab, 2022, 34(2):299-316.e6
Redox Biol, 2021, 46:102082
J Cell Mol Med, 2020, 24(6):3384-3398
S2075 Rosiglitazone (BRL-49653) HCl Rosiglitazone HCl (BRL-49653)是一种降血糖药物,通过在脂肪细胞中与PPAR受体结合而刺激胰岛素分泌。
Cell Death Dis, 2021, 12(11):972
Front Cell Dev Biol, 2021, 9:662868
Antioxidants (Basel), 2021, 10(2)155
S9199 Pseudoginsenoside F11 Pseudoginsenoside F11, a natural product found in American ginseng but not in Asian ginseng, is a novel partial PPARγ agonist.
S8770 Lanifibranor (IVA-337) Lanifibranor (IVA-337)是一种泛PPAR激动剂,对hPPARα、hPPARδ 和 hPPARγ的EC50值分别为1537 nM、866 nM和206 nM。
Brain Res Bull, 2021, 177:22-30
S3846 Eupatilin Eupatilin (NSC 122413), a major flavonoid from Artemisia plants, possesses various beneficial biological effects including anti-inflammation, anti-tumor, anti-cancer, anti-allergy, and anti-oxidation activity.
Clin Exp Reprod Med, 2020, 47(2):108-113
S3786 Glabridin Glabridin (Q-100692, KB-289522, LS-176045), one of the active phytochemicals in licorice extract, binds to and activates the ligand binding domain of PPARγ, as well as the full length receptor. It is also a GABAA receptor positive modulator promoting fatty acid oxidation and improving learning and memory.
Life Sci, 2021, S0024-3205(20)31752-5
S8432 Troglitazone (CS-045) Troglitazone (Rezulin, Romglizone, Prelay, CS045, Romozin) 是PPAR的有效激动剂,PPAR是配体激活的转录因,可参与调解细胞分化和生长。Troglitazone 诱导膀胱癌细胞自噬、凋亡和坏死。Troglitazone 可在Pfa1细胞中防止RSL3诱导的铁死亡和脂质过氧化。
Free Radic Biol Med, 2021, 163:234-242
Biomed Pharmacother, 2020, 132:110741
Nat Commun, 2019, 11;10(1):4621
S3878 Bavachinin Bavachinin (7-O-Methylbavachin) ia a novel natural pan-PPAR agonist from the fruit of the traditional Chinese glucose-lowering herb malaytea scurfpea. It shows stronger activities with PPAR-γ than with PPAR-α and PPAR-β/δ (EC50 = 0.74 μmol/l, 4.00 μmol/l and 8.07 μmol/l in 293T cells, respectively).
S0170 BMS-687453 BMS-687453 (compound 2) 是一种有效的 PPARα 的选择性激动剂,对人PPARα的EC50值为10 nM、IC50值为260 nM。
S5812 Choline Fenofibrate Choline fenofibrate是一种非诺贝特酸的胆碱盐,非诺贝特酸是一种合成的苯氧异丁酸衍生物,具有抗高血脂活性,是PPARα激动剂。
S9674 Saroglitazar Saroglitazar (Lipaglyn, ZYH1) 是一种 peroxisome proliferator-activated receptor (PPAR) 的激动剂,在HepG2细胞中对hPPARα和hPPARγ的EC50值分别为0.65 pM和3 nM。
S3720 Elafibranor Elafibranor (GFT505) 是PPAR-alphaPPAR-δ的激动剂,改善胰岛素敏感度、有益于葡萄糖稳态、脂质代谢并减少炎症。
S9480 Raspberry Ketone Raspberry ketone (p-Hydroxybenzyl acetone, Frambinone, Oxyphenylon, Rheosmin, Rasketone)是一种天然存在的酚类化合物,是红莓中的主要芳香化合物。
S5615 Cardarine Cardarine (GW501516, GW1516) is a synthetic PPARδ-specific agonist that displays high affinity for PPARδ (Ki=1.1 nM) with > 1000 fold selectivity over PPARα and PPARγ.
Cell Signal, 2022, 93:110304
J Lipid Res, 2014, 55(7):1254-66
S7955 EPI-001 EPI-001是androgen receptor N-端结构域的拮抗剂,也是一种选择性PPAR-gamma调节剂。
Prostate, 2019, 79(2):206-214
S3834 Astaxanthin Astaxanthin (β-Carotene-4,4'-dione, Trans-Astaxanthin), a xanthophyll carotenoid, is a nutrient with unique cell membrane actions and diverse clinical benefits with excellent safety and tolerability.
Aging (Albany NY), 2019, 11(22):10513-10531
Nature, 2018, 560(7718):372-376
S6906 Capric acid Capric acid (DA, Decanoic acid, Decylic acid) 是在椰子油和棕榈油中天然存在的中链甘油三酯的成分,可通过直接抑制 AMPA receptor 来控制癫痫发作。癸酸还是 PPARs 的调节配体。由于其特殊的熔化范围,产品可能是固体、液体或半固体状态。
S3868 Harmine Harmine (Telepathine) is an alkaloid of the β-carboline family that regulates PPARγ expression through inhibition of the Wnt signaling pathway. It also selectively binds to MAO-A and reversibly inhibits monoamine oxidase A (MAO-A) but not the variant MAO-B.
Cell Death Dis, 2019, 10(12):899
S2871 T0070907 T0070907是一种有效的,选择性PPARγ抑制剂,无细胞试验中IC50为1 nM,比作用于PPARα和PPARδ选择性高800倍以上。T0070907 在ME-180和SiHa细胞中可显著降低 DNA-PKcsRAD51 蛋白的表达水平。
Redox Biol, 2022, 50:102256
Biomed Pharmacother, 2022, 151:113109
Exp Neurol, 2022, 354:114100
S8046New GW7647 GW7647是一种有效的PPARα激动剂,对人PPARα、PPARγ和PPARδ的EC50分别为6 nM、1.1 μM和6.2 μM。
S7767 AZ6102 AZ6102是有效的TNKS1/2抑制剂,选择性比作用于其他PARP家族的激酶高100倍,其在DLD-1细胞中抑制Wnt信号通路(IC50为5 nM)。
Sci Adv, 2022, 8(19):eabh2332
Haematologica, 2021, 10.3324/haematol.2020.267096
Nat Commun, 2019, 10(1):4898
S2798 GW6471 GW 6471 是一种 PPARα 的有效拮抗剂,其IC50值为0.24 μM。
Cancer Discov, 2022, candisc.1181.2021
J Mol Endocrinol, 2022, JME-21-0239
Cell Rep, 2021, 37(6):109920
S7484 FH535 FH535是一种Wnt/β-catenin信号传导抑制剂,同时也是PPARγPPARδ的双重拮抗剂。
Cell Death Dis, 2022, 13(5):493
Sci Rep, 2022, 12(1):7
J Exp Clin Cancer Res, 2021, 40(1):230
S5824 Cinnamyl alcohol Cinnamyl alcohol是一种存在于肉桂中的天然产物。
S5113 Propyl gallate Propyl gallate (Gallic acid propyl esterZ, n-Propyl gallate) is an antioxidant used in foods especially animal fats and vegetable oils, also in a wide variety of cosmetics and beauty care products.
S4527 Fenofibric acid Fenofibric acid (NSC 281318, Trilipix, FNF acid)是一种降脂剂,降低低密度脂蛋白胆固醇和甘油三脂。
Int J Pharm, 2019, 570:118661
S9129 20(S)-Ginsenoside Rh1 20(S)-Ginsenoside Rh1 (Prosapogenin A2, Sanchinoside B2, Sanchinoside Rh1)是从红参中提取的主要生物活性化合物之一,在世界范围内,红参已越来越多地用于增强认知和身体健康。它具有抗发炎、抗氧化、免疫调节作用和对神经系统有积极作用的有效特性。20(S)-Ginsenoside Rh1 可抑制 PPAR-γTNF-αIL-6IL-1β 的表达。
S7867 Oleuropein Oleuropein 是一种从橄榄叶中分离出的抗氧化多酚。Oleuropein 具有抗氧化、抗炎和抗动脉粥样硬化的作用,并在体外抑制脂肪细胞的分化。Oleuropein 抑制 PPARγ 活性。Oleuropein 通过直接抑制PPARγ转录活性发挥抗脂肪形成作用。Oleuropein 还可抑制aromatase。Oleuropein 可诱导凋亡。Phase 2。
J Med Virol, 2019, 91(8):1440-1447
E0473New CUDA CUDA是一种有效的可溶性环氧化物水解酶(soluble epoxide hydrolase, sEH)抑制剂,对小鼠和人sEH的IC50s分别为11.1 nM和112 nM,也能选择性地增加过氧化物酶体增殖物激活受体(peroxisome proliferator-activated receptor alpha, PPAR alpha)的活性。
S8029 WY-14643 (Pirinixic Acid) WY-14643 (Pirinixic Acid, NSC 310038) 是一种有效的选择性 PPARα 激活剂,EC50 为 1.5 μM。
Haematologica, 2021, 10.3324/haematol.2021.279770
Free Radic Biol Med, 2021, 169:283-293
Aging (Albany NY), 2021, 13(8):11969-11987
S1729 Gemfibrozil Gemfibrozil (CI-719) 是一种降低血脂水平的化合物。
S1849 Daidzein Daidzein属于异黄酮类。
J Mol Neurosci, 2018, 64(2):211-223
S9189 Oroxin A Oroxin A (Baicalein 7-O-glucoside), an active component isolated from the herb Oroxylum indicum (L.) Kurz, activates PPARγ and inhibits α-glucosidase, exerting antioxidant activity.
S3290 Procyanidin B2 Procyanidin B2 (PCB2) 是一种存在于常见食品中的天然类黄酮,具有抗炎、抗氧化和抗癌活性。Procyanidin B2 可激活 PPARγ 并诱导小鼠巨噬细胞M2极化。Procyanidin B2 可显著抑制百草枯在大鼠模型中肺组织中 NLRP3 炎性小体的活化。
S9723 CDDO-Im CDDO-Im (CDDO-Imidazolide, RTA-403, TP-235) 是一种 nuclear factor erythroid 2–related factor 2 (Nrf2)peroxisome proliferator-activated receptor (PPAR) 的激活剂。CDDO-Im 可与PPARα和PPARγ结合,对应的Ki值分别以232 nM和344 nM。CDDO-Im 在体内抑制炎症反应和肿瘤生长。
S5121 Phytol Phytol (Trans-Phytol), a diterpene alcohol from chlorophyll widely used as a food additive and in medicinal fields, shows antinociceptive and antioxidant activities as well as anti-inflammatory and antiallergic effects. It is a specific activator of PPARα.
S3875 Alpinetin Alpinetin, a composition of Alpinia katsumadai Hayata, has been reported to have a number of biological properties, such as antibacterial, antitumor and other important therapeutic activities.
Nutrients, 2021, 13(10)3382
S5851 4'-Methoxychalcone 4'-Methoxychalcone存在于柑橘属植物中,是一种查耳酮衍生物,具有多种药理活性,如抗肿瘤和消炎活性。
S4708 Palmitoylethanolamide Palmitoylethanolamide (PEA, Palmidrol, N-palmitoylethanolamine) 是一种内源性的脂肪酸酰胺,能在体外选择性激活PPAR-α,EC50为3.1±0.4 μM。
Neurosci Insights, 2020, 15:2633105520975412
J Steroid Biochem Mol Biol, 2019, 10.1016/j.jsbmb.2018.07.005
S9177 Gypenoside XLIX Gypenoside XLIX, a naturally occurring gynosaponin, is a selective peroxisome proliferator-activated receptor (PPAR)-alpha activator.
S2915 GW9662 GW9662是一种选择性PPAR拮抗剂,作用于PPARγ,无细胞试验中IC50为3.3 nM,在细胞中作用于PPARγ比作用于PPARα和PPARδ的功能选择性强10到600倍。
Brain Behav Immun, 2022, S0889-1591(22)00025-3
Free Radic Biol Med, 2022, 186:1-16
Oxid Med Cell Longev, 2022, 2022:9226022
S8025 GSK3787 GSK3787是一种选择性的,不可逆PPARδ拮抗剂,pIC50为6.6,对hPPARα和hPPARγ没有亲和力。
Cancer Discov, 2022, candisc.1181.2021
J Mol Endocrinol, 2022, JME-21-0239
Cell Death Dis, 2021, 12(3):240
S0531 DG172 dihydrochloride DG-172 dihydrochloride是一种新型的PPARβ/δ选择性拮抗剂,IC50为27 nM。
Cell Signal, 2022, 93:110304
S0773 Mifobate Mifobate (SR-202)是一种有效的特异性PPARγ拮抗剂,可选择性地抑制噻唑烷二酮(TZD)诱导的PPARγ转录活性(IC50=140 μM)。
S5817 GSK0660 GSK0660是有效的PPARβ/δ拮抗剂,pIC50为6.8。在浓度高达近于10 μM时,对PPARα和PPARγ没有活性。
Nat Commun, 2019, 11;10(1):4621
S2505 Rosiglitazone (BRL-49653) maleate Rosiglitazone maleate (BRL 49653) 是一种噻唑烷二酮类抗高血糖药,是PPARγ的高亲和、选择性的激动剂,IC50为42 nM。Rosiglitazone maleate 也能调节 TRP channels并诱导自噬。Rosiglitazone 可预防铁死亡。
Cell Death Dis, 2021, 12(11):972
Antioxidants (Basel), 2021, 10(2)155
Front Cardiovasc Med, 2021, 8:698056
S2556 Rosiglitazone (BRL 49653) Rosiglitazone (BRL 49653) 是有效的降糖药,也是有效的噻唑烷二酮类胰岛素增敏剂,在大鼠,3T3-L1和人体脂肪细胞中IC50分别为12,4和9 nM。Rosiglitazone是PPAR-gamma的配体,对PPAR-alpha没有结合力。Rosiglitazone 可调控 TRP channels 并诱导自噬。Rosiglitazone可阻止铁死亡。
Redox Biol, 2022, 50:102256
Toxicology, 2022, 465:153048
Hum Cell, 2022, 10.1007/s13577-022-00671-y
S2590 Pioglitazone (AD-4833) Pioglitazone (AD-4833, U 72107)是一种选择性过氧化物酶体增殖物激活受体γ (PPARγ) 激动剂, 用于治疗糖尿病。是全长hPPARα的弱激活剂,对全长hPPARδ没有作用。
Commun Biol, 2022, 5(1):231
Exp Neurol, 2022, 354:114100
J Genet Genomics, 2022, S1673-8527(22)00133-3
S8020 GW0742 GW0742是一种有效的,选择性PPARβ/δ激动剂,IC50为1 nM,比作用于hPPARα和hPPARγ选择性高1000倍。
Life Sci, 2021, 279:119696
Cells, 2019, 8(12)
Int J Med Sci, 2019, 16(12):1593-1603
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
Cell Immunol, 2022, 378:104556
S2665 Ciprofibrate Ciprofibrate (Win-35833)是一种过氧化物酶体增殖物激活受体激动剂。
Respir Physiol Neurobiol, 2020, 271:103290
S4159 Bezafibrate Bezafibrate (BM 15075) 是第一个临床测试的双重pan-peroxisome proliferator-activated receptors (PPAR)(过氧化物酶体增殖物激活受体)联合激动剂。
Nat Commun, 2021, 12(1):1929
PPAR Res, 2021, 2021:5589342
S4207 Clofibric Acid Clofibric acid 是PPARα激动剂,是一种降血脂剂。
S1794 Fenofibrate (NSC-281319) Fenofibrate (NSC-281319)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。
Cell Metab, 2022, 34(2):299-316.e6
Redox Biol, 2021, 46:102082
J Cell Mol Med, 2020, 24(6):3384-3398
S2075 Rosiglitazone (BRL-49653) HCl Rosiglitazone HCl (BRL-49653)是一种降血糖药物,通过在脂肪细胞中与PPAR受体结合而刺激胰岛素分泌。
Cell Death Dis, 2021, 12(11):972
Front Cell Dev Biol, 2021, 9:662868
Antioxidants (Basel), 2021, 10(2)155
S9199 Pseudoginsenoside F11 Pseudoginsenoside F11, a natural product found in American ginseng but not in Asian ginseng, is a novel partial PPARγ agonist.
S8770 Lanifibranor (IVA-337) Lanifibranor (IVA-337)是一种泛PPAR激动剂,对hPPARα、hPPARδ 和 hPPARγ的EC50值分别为1537 nM、866 nM和206 nM。
Brain Res Bull, 2021, 177:22-30
S3846 Eupatilin Eupatilin (NSC 122413), a major flavonoid from Artemisia plants, possesses various beneficial biological effects including anti-inflammation, anti-tumor, anti-cancer, anti-allergy, and anti-oxidation activity.
Clin Exp Reprod Med, 2020, 47(2):108-113
S3786 Glabridin Glabridin (Q-100692, KB-289522, LS-176045), one of the active phytochemicals in licorice extract, binds to and activates the ligand binding domain of PPARγ, as well as the full length receptor. It is also a GABAA receptor positive modulator promoting fatty acid oxidation and improving learning and memory.
Life Sci, 2021, S0024-3205(20)31752-5
S8432 Troglitazone (CS-045) Troglitazone (Rezulin, Romglizone, Prelay, CS045, Romozin) 是PPAR的有效激动剂,PPAR是配体激活的转录因,可参与调解细胞分化和生长。Troglitazone 诱导膀胱癌细胞自噬、凋亡和坏死。Troglitazone 可在Pfa1细胞中防止RSL3诱导的铁死亡和脂质过氧化。
Free Radic Biol Med, 2021, 163:234-242
Biomed Pharmacother, 2020, 132:110741
Nat Commun, 2019, 11;10(1):4621
S3878 Bavachinin Bavachinin (7-O-Methylbavachin) ia a novel natural pan-PPAR agonist from the fruit of the traditional Chinese glucose-lowering herb malaytea scurfpea. It shows stronger activities with PPAR-γ than with PPAR-α and PPAR-β/δ (EC50 = 0.74 μmol/l, 4.00 μmol/l and 8.07 μmol/l in 293T cells, respectively).
S0170 BMS-687453 BMS-687453 (compound 2) 是一种有效的 PPARα 的选择性激动剂,对人PPARα的EC50值为10 nM、IC50值为260 nM。
S5812 Choline Fenofibrate Choline fenofibrate是一种非诺贝特酸的胆碱盐,非诺贝特酸是一种合成的苯氧异丁酸衍生物,具有抗高血脂活性,是PPARα激动剂。
S9674 Saroglitazar Saroglitazar (Lipaglyn, ZYH1) 是一种 peroxisome proliferator-activated receptor (PPAR) 的激动剂,在HepG2细胞中对hPPARα和hPPARγ的EC50值分别为0.65 pM和3 nM。
S3720 Elafibranor Elafibranor (GFT505) 是PPAR-alphaPPAR-δ的激动剂,改善胰岛素敏感度、有益于葡萄糖稳态、脂质代谢并减少炎症。
S9480 Raspberry Ketone Raspberry ketone (p-Hydroxybenzyl acetone, Frambinone, Oxyphenylon, Rheosmin, Rasketone)是一种天然存在的酚类化合物,是红莓中的主要芳香化合物。
S5615 Cardarine Cardarine (GW501516, GW1516) is a synthetic PPARδ-specific agonist that displays high affinity for PPARδ (Ki=1.1 nM) with > 1000 fold selectivity over PPARα and PPARγ.
Cell Signal, 2022, 93:110304
J Lipid Res, 2014, 55(7):1254-66
S7955 EPI-001 EPI-001是androgen receptor N-端结构域的拮抗剂,也是一种选择性PPAR-gamma调节剂。
Prostate, 2019, 79(2):206-214
S3834 Astaxanthin Astaxanthin (β-Carotene-4,4'-dione, Trans-Astaxanthin), a xanthophyll carotenoid, is a nutrient with unique cell membrane actions and diverse clinical benefits with excellent safety and tolerability.
Aging (Albany NY), 2019, 11(22):10513-10531
Nature, 2018, 560(7718):372-376
S6906 Capric acid Capric acid (DA, Decanoic acid, Decylic acid) 是在椰子油和棕榈油中天然存在的中链甘油三酯的成分,可通过直接抑制 AMPA receptor 来控制癫痫发作。癸酸还是 PPARs 的调节配体。由于其特殊的熔化范围,产品可能是固体、液体或半固体状态。
S3868 Harmine Harmine (Telepathine) is an alkaloid of the β-carboline family that regulates PPARγ expression through inhibition of the Wnt signaling pathway. It also selectively binds to MAO-A and reversibly inhibits monoamine oxidase A (MAO-A) but not the variant MAO-B.
Cell Death Dis, 2019, 10(12):899
S8046New GW7647 GW7647是一种有效的PPARα激动剂,对人PPARα、PPARγ和PPARδ的EC50分别为6 nM、1.1 μM和6.2 μM。
E0473New CUDA CUDA是一种有效的可溶性环氧化物水解酶(soluble epoxide hydrolase, sEH)抑制剂,对小鼠和人sEH的IC50s分别为11.1 nM和112 nM,也能选择性地增加过氧化物酶体增殖物激活受体(peroxisome proliferator-activated receptor alpha, PPAR alpha)的活性。
Tags: PPAR inhibitor|PPAR agonist|PPAR activator|PPAR inducer|PPAR antagonist|PPAR signaling pathway|PPAR assay kit