Calcium Channel

Calcium Channel抑制剂选择性比较

Calcium Channel信号通路图

Calcium Channel信号通路图

Calcium Channel产品

  • 所有产品(91)
  • Calcium Channel抑制剂 (66)
  • Calcium Channel激活剂 (3)
  • Calcium Channel拮抗剂 (7)
  • Calcium Channel激动剂 (3)
  • Calcium Channel调节剂 (8)
目录号 产品名 产品描述 文献引用 实验数据
S1573 Fasudil (HA-1077) HCl Fasudil (HA-1077, AT-877)是一种有效的、具有选择性的Rho抑制剂(ROCK2, Ki=0.33 μM),同时对PKA、PKG、PKC和MLCK也具有抑制活性,Ki值分别为1.6 μM、1.6 μM、3.3 μM、36 μM。Fasudil 也是calcium channel的阻滞剂。
Aging Cell, 2022, e13587
Cell Death Dis, 2022, 13(2):138
iScience, 2022, 25(6):104398
S1356 Levetiracetam (UCB-L059) Levetiracetam (UCB-L059, SIB-S1) 是一种抗癫痫化合物。Levetiracetam (UCB-L059, SIB-S1) 是 muscarinic acetylcholine receptors (mAChR) 的激动剂并能调节突触前P/Q型压敏钙离子通道 calcium (Ca2+) channel
Anticancer Res, 2021, 41(2):687-697
PLoS One, 2019, 14(2):e0211644
Sci Rep, 2016, 6:25705
S1813 Amlodipine Besylate Amlodipine Besylate是一种长效的钙离子通道抑制剂,IC50为1.9 nM。
Cell Discov, 2020, 6(1):96
Oncogene, 2019, 38(1):120-139
S1293 Cilnidipine (FRC-8653) Cilnidipine (FRC-8653) 是一种L型和N型钙离子通道抑制剂,用来治疗高血压。
ACS Infect Dis, 2020, acsinfecdis.0c00486
Cell Discov, 2020, 6(1):96
Res Sq, 2020, rs.3.rs-48659
S1811 Amiloride (MK-870) HCl Amiloride (MK-870)是一种选择性的T-type calcium channel阻滞剂,epithelial sodium channel(ENaC)阻滞剂,urokinase plasminogen activator (uPA)抑制剂,Ki=7 μM。
Mol Ther Methods Clin Dev, 2022, 24:11-19
Adv Sci (Weinh), 2021, 8(13):2100962
Theranostics, 2021, 11(5):2364-2380
E0778New o-3M3FBS O-3M3FBS是m-3M3FBS的阴性对照,以独立于PLC的机制及拮抗的方式抑制内向和外向电流,可逆地抑制延迟整流K+通道,以与m-3M3FBS竞争的形式增加[Ca2+](i)
E0826New Levamlodipine Besylate Levamlodipine Besylate是一种强大的二氢吡啶钙通道(dihydropyridine calcium channel)阻滞剂,具有血管舒张特性,用于高血压和心绞痛的治疗。
S1425 Ranolazine 2HCl Ranolazine 2HCl (RS-43285)是一种钙离子通过 sodium/calcium channal摄取的抑制剂抗心绞痛药物,用于治疗慢性心绞痛。
Front Pharmacol, 2019, 10:1367
S4202 Verapamil (CP-16533-1) HCl Verapamil HCl (CP-16533-1)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
EMBO Mol Med, 2022, 14(2):e14903
Cell Rep, 2022, 38(10):110468
ACS Nano, 2021, 10.1021/acsnano.1c03517
S2482 Manidipine 2HCl Manidipine 2HCl (CV-4093) 是Manidipine的盐酸盐形式,是钙通道阻断剂,IC50为2.6 nM,临床上常用于抗高血压。Phase 4。
Environ Toxicol Chem, 2021, 10.1002/etc.5018
S1799 Ranolazine Ranolazine (CVT 303, RS 43285-003)是一种钙离子通过 sodium/calcium channal摄取的抑制剂抗心绞痛药物,用于治疗慢性心绞痛。
S1662 Isradipine Isradipine (PN 200-110)是一种高效选择性的L型压力控式钙离子通道抑制剂,用于治疗高血压。
Environ Toxicol Chem, 2021, 10.1002/etc.5018
Cell Discov, 2020, 6(1):96
Drug Metab Dispos, 2015, 43(12):1934-7
S1905 Amlodipine Amlodipine (UK-48340) 是一种长效的钙离子通道抑制剂,用于降低血压缓解胸部疼痛。
Oncogene, 2021, 40(6):1128-1146
ACS Infect Dis, 2020, acsinfecdis.0c00486
J Med Toxicol, 2020, 16(1):61-66
S1885 Felodipine Felodipine (CGH-869) 是一种选择性L型Ca2+通道阻断剂,IC50为0.15 nM。
ACS Infect Dis, 2020, acsinfecdis.0c00486
Cell Discov, 2020, 6(1):96
S2481 Manidipine Manidipine是一种二氢吡啶类钙拮抗剂,用于治疗高血压。
Antiviral Res, 2018, 150:130-136
S1748 Nisoldipine Nisoldipine (Sular, BAY K 5552)是特定L型CaV1.2钙通道阻断剂,IC50为10 nM。
Biomed Pharmacother, 2022, 145:112432
Cell Mol Gastroenterol Hepatol, 2021, S2352-345X(21)00196-X
Cell Discov, 2020, 6(1):96
S1747 Nimodipine Nimodipine (BAY E 9736) 是一种二氢吡啶衍生物,是钙离子通道抑制剂Nifedipine的类似物,具有降压活性。Nimodipine能减少细胞内游离Ca2+,Beclin-1及细胞自噬。
Cell Discov, 2020, 6(1):96
G3 (Bethesda), 2020, 4;10(5):1585-1597
Antiviral Res, 2016, 132:38-45
S2721 Nilvadipine Nilvadipine (ARC029, FR34235) 是一种强效钙通道阻滞剂,IC50为0.03 nM。
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Hum Cell, 2021, 10.1007/s13577-021-00639-4
Hum Cell, 2021, 34(6):1911-1918
S1994 Lacidipine Lacidipine (GX-1048, GR-43659X, SN-305)是一种L-型钙离子通道抑制剂。
S2114 Dronedarone HCl Dronedarone HCl (SR33589) 用于治疗阵发性和持续性房颤或房扑的患者。
Chem Res Toxicol, 2021, 10.1021/acs.chemrestox.1c00127
Cell Syst, 2019, 8(2):97-108
Nat Commun, 2016, 7:13023
S4181 Nicardipine HCl Nicardipine HCl (RS-69216)是二氢吡啶的钙通道抑制剂,具有显著的血管扩张作用。
ACS Infect Dis, 2020, acsinfecdis.0c00486
Cell Discov, 2020, 6(1):96
S1808 Nifedipine (BAY-a-1040) Nifedipine (BAY-a-1040)是一种二氢吡啶类钙离子通道阻滞剂,是有效的血管扩张剂,具有钙拮抗作用。
Oncogene, 2021, 40(6):1128-1146
Cell Discov, 2020, 6(1):96
Front Pharmacol, 2019, 10:381
S2080 Clevidipine Butyrate Clevidipine Butyrate是一种二氢吡啶类钙离子通道抑制剂,用于降血压。
ACS Infect Dis, 2020, acsinfecdis.0c00486
S2017 Benidipine HCl Benidipine HCl (KW-3049) 是Benidipine的盐酸盐形式,是一种二氢吡啶类的钙离子通道抑制剂。 
ACS Infect Dis, 2020, acsinfecdis.0c00486
Cell Discov, 2020, 6(1):96
Life Sci, 2019, 227:74-81
S2030 Flunarizine 2HCl Flunarizine 2HCl (KW-3149, R14950) 是一种二氢盐酸盐,抑制钙离子通道,Ki为68 nM。
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Hum Cell, 2021, 10.1007/s13577-021-00639-4
Hum Cell, 2021, 34(6):1911-1918
S2491 Nitrendipine Nitrendipine (Bayotensin) 是一种二氢吡啶类钙离子通道抑制剂,IC50为95 nM。
S3053 Azelnidipine Azelnidipine (UR-12592)是一种二氢吡啶类钙通道阻断剂。
Cell Mol Gastroenterol Hepatol, 2021, S2352-345X(21)00196-X
Environ Toxicol Chem, 2021, 10.1002/etc.5018
S2573 Tetracaine HCl Tetracaine HCl (Amethocalne)是Tetracaine的盐酸盐形式,是一种有效的局部麻醉剂和通道功能变构酶抑制剂。
S0000 Cav 2.2 blocker 1 Cav 2.2 blocker 1 (compound 9) 是一种 N-type calcium channel (Cav 2.2) 阻滞剂可用于治疗疼痛,其IC50值为0.001 μM。
S1865 Diltiazem HCl Diltiazem (Tiazac, RG 83606) HCl 是一种Benzothiazepine衍生物,具有舒张血管的作用,由于其抑制钙离子在膜的功能。
J Cell Mol Med, 2018, 22(12):5964-5977
FASEB J, 2017, 31(2):625-635
S3045 Cinepazide maleate Cinepazide maleate是cinepazide的马来酸盐形式,而cinepazide是一种血管舒张药。
S5255 Nicardipine Nicardipine is a potent calcium channel blockader with marked vasodilator action.
Cell Chem Biol, 2021, S2451-9456(21)00442-6
S3242 Loureirin B Loureirin B (LB, LrB),是从Dracaena cochinchinensis中提取的类黄酮,是 PAI-1 的抑制剂,其IC50值为26.10 μM。Loureirin B 可下调TGF-β1刺激的成纤维细胞中的 p-ERKp-JNK。Loureirin B 主要通过增加Pdx-1、MafA、细胞内ATP水平来促进胰岛素分泌,抑制 KATP 电流,Ca2+ 进入细胞内。
S8380 YM-58483 (BTP2) YM-58483/BTP2是钙池调控钙离子进入(SOCE)的阻滞剂,参与调解不可兴奋细胞如淋巴细胞的激活。
Dev Cell, 2022, S1534-5807(21)01035-2
Front Pharmacol, 2021, 12:622774
Cell Stem Cell, 2018, 22(6):865-878
S0535 FK962 FK962是FK960的衍生物,具有抗痴呆的特性,在1-1000 nM时,显著增强高K+诱导的大鼠海马片的生长抑素释放,在1-100 nM时,也显著降低生长抑素诱导的大鼠海马神经元的Ca2+通道抑制。
S6657 2-Aminoethyl Diphenylborinate (2-APB) 2-Aminoethyl Diphenylborinate (2-APB)是IP3 receptor的抑制剂,可以调节IP3诱导的钙释放。2-APB还可以抑制SOC通道的活性,并且在高浓度的时候可以激活TRP通道
Int J Biol Sci, 2021, 17(13):3672-3688
Int J Biol Sci, 2021, 17(13):3672-3688
Chem Biol Interact, 2021, 351:109756
S4626 Ethosuximide Ethosuximide是一种琥珀酰亚胺类的抗痉挛试剂,主要用于失神发作。是钙离子通道阻滞剂。
Nature, 2018, 554(7692):317-322
S5966 Amlodipine maleate Amlodipine (Amvaz, UK-48340) maleate 是一种长效的 calcium channel 的阻滞剂,可用于降低血压或预防胸痛。
S4597 Lercanidipine hydrochloride Lercanidipine是二氢吡啶类的钙离子通道抑制剂。
J Phys Chem B, 2013, 117(23):6868-73
S4977 Efonidipine Efonidipine (NZ-105) 是一种L型和T型钙离子通道阻滞剂,可引起血管舒张和心脏自律性降低。它还能抑制醛固酮从肾上腺分泌。
S5279 Fendiline hydrochloride Fendiline hydrochloride is the hydrochloride salt form of Fendiline, which is an L-type calcium channel blocker and also a specific inhibitor of K-Ras plasma membrane targeting with no detectable effect on the localization of H- and N-Ras.
S3845 Panaxadiol Panaxadiol (20(R)-Panaxadiol) is a triterpene sapogenin originally found in species of Panax (ginseng) and exhibits anticancer, cardioprotective, anti-arrhythmic, and antioxidative activities. It inhibits Ca2+ channels, decreasing channel open time and open state probability in vitro and displaying anti-arrhythmic potential.
S5898 Efonidipine hydrochloride monoethanolate Efonidipine (NZ-105) hydrochloride monoethanolate 是一种L型和T型 calcium channel 的阻滞剂,可导致血管舒张并降低心脏的自动节律性。Efonidipine hydrochloride monoethanolate 还抑制肾上腺醛固酮的分泌。
S3700 DHBP dibromide DHBP (1,1'-diheptyl-4,4'-bipyridinium),一种用于电致色记忆显示剂的紫罗碱,抑制由2 mM咖啡因和2 μg/ml多熔素诱导的钙释放,IC50分别为5 μg/ml和4 μg/ml。
S6834 CM 4620 CM 4620 是一种 calcium-release activated calcium-channel (CRAC channel) 的抑制剂。CM4620 抑制Orai1/STIM1介导的Ca2+电流和Orai2/STIM1介导的电流,对应的IC50值分别接近120 nM和900 nM。
S9017 Columbianadin Columbianadin (Zosimin, 2-Butenoic acid) 是一种来自当归的天然香豆素,已知具有多种生物活性,包括钙通道阻断活性、对各种癌细胞系的细胞毒活性、镇痛活性、肠道吸收和运输、抗炎和抗癌作用。
S2403 Tetrandrine (NSC-77037) Tetrandrine (NSC-77037, Fanchinine, d-Tetrandrine)是来源于千金藤根部的一种双苯基异喹啉,一种钙离子通道抑制剂。
FASEB J, 2021, 35(5):e21502
Nat Commun, 2020, 27;11(1):1620
Ann Transl Med, 2020, 8(16):1018
S9315 Praeruptorin A Praeruptorin A, a naturally existing pyranocumarin, is isolated from the dried root of Peucedanum praeruptorum Dunn. Praeruptorin A inhibits p38/Akt-c-Fos-NFATc1 signaling and PLCγ-independent Ca2+ oscillation. Praeruptorin A can significantly upregulates multidrug resistance-associated protein 2 expression via the constitutive androstane receptor-mediated pathway in vitro, and this should be taken as an herb-drug interaction.
S6920 SEA0400 SEA0400 是一种选择性的 Na+-Ca2+ exchanger (NCX) 的强效抑制剂,可抑制神经细胞、星形胶质细胞和小胶质细胞中Na+依赖性的Ca2+吸收,对应的IC50值分别为33 nM、5.0 nM和8.3 nM。SEA0400 可防止硝普钠 (SNP) 提高 ERKp38 MAPK 的磷酸化和通过细胞外Ca2+依赖的方式增强reactive oxygen species (ROS) 的产生。
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.
J Ethnopharmacol, 2021, S0378-8741(21)00169-0
S5514 Lanthanum(III) chloride heptahydrate Lanthanum(III) chloride is the inorganic compound used in biochemical research to block the activity of divalent cation channels, mainly calcium channels.
J Surg Res, 2021, 263:236-244
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).
S4084 Lomerizine 2HCl Lomerizine dihydrochloride (KB-2796) 是一种相对较新的L-和T-型钙通道阻滞剂,用于治疗偏头痛。
S4648 Dantrolene sodium hemiheptahydrate Dantrolene sodium hemiheptahydrate (Dantrium) 是一种骨骼肌松弛药,通过干扰肌纤维中的兴奋-收缩偶联起作用。
Cardiovasc Res, 2021, 117(4):1091-1102
Oxid Med Cell Longev, 2021, 2021:8810698
S3682 Ethyl 3-Aminobenzoate methanesulfonate Ethyl 3-Aminobenzoate (Ethyl m-Aminobenzoate, NSC 93790, Tricaine) 可通过voltage-dependent Na+-channels阻止动作电位的产生,常用于鱼类的麻醉、镇静和安乐死。
S9400 Rhynchophylline Rhynchophylline (Mitrinermine), an active component isolated from species of the genus Uncaria, acts as a calcium channel blocker and is widely used in traditional Chinese medicine mainly for treating ailments of central nervous and cardiovascular systems, such as lightheadedness, convulsions, numbness, and hypertension.
S3674 Levamlodipine Levamlodipine (S-amlodipine) is a pharmacologically active enantiomer of amlodipine which belongs to the dihydropyridine group of calcium channel blocker. It acts on the L-type of calcium channels and its treatment results in vasodilation and a fall in blood pressure.
Oncogene, 2021, 40(6):1128-1146
S3883 Protopine Protopine (Corydinine, Fumarine, Biflorine, Macleyine), an alkaloid present in different plants, has been shown to exhibit a number of activities, such as inhibition of calcium influx through both voltage and receptor-operated channels and inhibition of rabbit blood platelet aggregation. It also possesses anti-cholinergic and anti-histaminic as well as anti-bacterial activities.
S5567 Trimethadione Trimethadione is an oxazolidinedione anticonvulsant and often used to treat epileptic conditions that are resistant to other treatments.
S9566 Bepridil hydrochloride Bepridil hydrochloride是一种抗心绞痛的药物,是钙离子通道(calcium channel)阻滞剂。它能阻止多种其他离子通道,包括钠离子和钾离子通道。
S6847 ML-9 HCl ML-9 HCl (ML-9 hydrochloride) 是一种有效的选择性的 Akt kinasemyosin light chain kinase (MLCK)stromal interaction molecule 1 (STIM1)。ML-9 HCl 也是 Ca2+-permeable channels 的有效抑制剂。ML-9 HCl 是一种靶向自噬和细胞死亡的亲溶酶体剂。
J Mol Endocrinol, 2019, 63(3):199-213
S0452 NP118809 NP118809(39-1B4)是一种有效的N型钙通道(N-type calcium channel)阻滞剂,IC50为0.11 μM,对L型钙通道(L-type calcium channel)的抑制作用也较弱,IC50为12.2 μM。
S0016 SN-6 SN-6 是一种选择性的 Na+/Ca2+ exchanger (NCX) 抑制剂。SN-6 可抑制NCX1、NCX2和NCX3,对应的IC50值分别为2.9 μM、16 μM和8.6 μM。SN-6 可消除 acetylcholine (ACh) 诱导的血管舒张。
S6473 Pinaverium bromide Pinaverium bromide (Icosapentaenoic acid)是calcium channel阻滞剂,适用于治疗功能性胃肠病。
S4727 Cinnarizine Cinnarizine (Stugeron, Dimitronal, Stutgin, Cinarizine)是piperazine的药物衍生物,是抗组胺剂钙离子通道阻滞剂。
S9842 MCU-i4 MCU-i4 是 mitochondrial calcium uniporter (MCU) 复合物的负调节剂,可直接结合 MICU1 中的特定裂缝并减少线粒体 Ca2+ 流入。
S2050 Strontium Ranelate Strontium Ranelate 是Ranelic acid的锶(II)盐,用于(-)-Desmethoxyverapamil结合到钙离子通道,IC50为0.5 mM。
S7924 Bay K 8644 Bay K 8644是一种高选择性的L型钙离子通道激动剂,EC50为17.3 nM。
ACS Nano, 2021, 10.1021/acsnano.1c03517
Cell Biol Toxicol, 2021, 10.1007/s10565-021-09615-y
Journal of Advanced Research, 2020, 10.1016/j.jare.2020.10.005
S4209 Chlorocresol Chlorocresol 是ryanodine receptor激活剂。
E0777New Z944 Z944是一种高度选择性的T型钙通道拮抗剂,对hCaV3.1、hCaV3.2和hCaV3.3的IC50分别为50、160、110 nM。
E0945New BIA BIA (TMBIM6 antagonist BIA)是一个潜在的TMBIM6拮抗剂,可以阻断TMBIM6和mTORC2的相互作用,最终阻断AKT的激活和癌症进展。
S4931 Propiverine hydrochloride Propiverine是一种抗胆碱能药物,用于治疗膀胱过度活动症和尿失禁。
S0870 Barnidipine Barnidipine (Libradin, Mepirodipine, Vasexten, YM-09730-5, Cyress, Hypoca, Oldeca) 是一种降压药,属于dihydropyridine (DHP)组的calcium 拮抗剂 (CaA),对[3H]nitrendipine 结合位点的Ki值为0.21 nM。
S3809 Imperatorin Imperatorin (Ammidin, Marmelosin, Pentosalen, 8-Isoamylenoxypsoralen), a naturally occurring psoralen-type furanocoumarin, is a potent myorelaxant agent and acts as a calcium antagonist on vascular smooth muscle.
Front Cell Dev Biol, 2020, 8:592433
Adv Sci (Weinh), 2020, 7(16):2000925
Theriogenology, 2019, 10.1016/j.theriogenology
S2436 Pranidipine Pranidipine (Acalas, OPC 13340)是一种新型的1,4-二氢吡啶 calcium channel 阻滞剂。Pranidipine可以增强cyclic GMP依赖性一氧化氮诱导的大鼠主动脉舒张。
S5861 Lercanidipine Lercanidipine是一种对血管具有特异性的钙离子通道拮抗剂,可用于治疗发性高血压。
E0137New GV-58 GV-58 是一种新型的选择性 N 型和 P/Q 型 Ca2+ 通道激动剂,IC50 分别为 7.21 μM 和 8.81 μM。
S5191 Cinacalcet Cinacalcet (AMG073, Sensipar, Cin) 是一种口服活性的 receptors for calcium (CaR) 的变构激动剂,可增加CaR对Ca的敏感性。
Int J Mol Sci, 2022, 23(8)4323
S9151 Praeruptorin E Praeruptorin E, isolated from Peucedanum praeruptorum Dunn., is a cardiotonic agent with selective cardiac calcium channel agonistic effect.
E0936New IGS-1.76 IGS-1.76是一种蛋白-蛋白相互作用(protein-protein interaction, PPI)抑制剂,具有药物样特性,对人类神经钙传感蛋白1(human neuronal calcium sensor 1, hNCS-1)具有显著的亲和力,并有效地调节hNCS-1和鸟嘌呤交换因子Ric8a的相互作用。
S2535 Econazole nitrate Econazole Nitrate (NSC 243115) 是一种咪唑类抗真菌药物。
Biomol Ther (Seoul), 2020, 25
S0713 S107 hydrochloride S107 hydrochloride 是一种 RyR2 (type 2 ryanodine receptor)/FKBP12.6 (FK506 binding protein 12.6) complex 的特异性稳定剂,会影响 Ca2+ 信号传导。
S3236 Mesaconitine Mesaconitine 是Aconiti tuber附子块茎中的附子生物碱之一,通过从细胞外空间流入Ca2+来增加内皮细胞中的[Ca2+]i水平。
S0973 Wilforgine Wilforgine 是 Tripterygium wilfordii Hook. F.中主要的生物活性倍半萜生物碱之一,可在M. separata larvae的肌肉中诱导显微结构和超微结构变化,其发挥作用的位置是肌肉系统中的 calcium receptors or channels
S2415 Astragaloside A Astragaloside A是从黄芪中分离的一种纯化的皂苷,广泛应用于治疗心血管疾病。
Sci Rep, 2022, 12(1):7
Carcinogenesis, 2020, 41(7):993-1004
J Med Virol, 2019, 91(8):1440-1447
S3191 Azumolene Azumolene(EU4093 free base)是一种等效的丹曲林(dantrolene)类似物,是一种兰尼碱受体 (ryanodine receptor, RyR) 调节剂,可抑制钙释放。
S4353 Terfenadine Terfenadine is an antihistamine, generally completely metabolizes to the active form fexofenadine in the liver by the enzyme cytochrome P450 CYP3A4 isoform. Terfenadine ((±)-Terfenadine) is a potent open-channel blocker of hERG with an IC50 of 204 nM. Terfenadine, an H1 histamine receptor antagonist, acts as a potent apoptosis inducer in melanoma cells through modulation of Ca2+ homeostasis. Terfenadine induces ROS-dependent apoptosis, simultaneously activates Caspase-4, -2, -9.
S2446 Levosimendan Levosimendan 是一种钙增敏剂,通过与cardiac troponin C (cTnC)结合而发挥作用,这种作用具有钙依赖性。
Antiviral Res, 2017, 146:76-85
S1911 Disodium Cromoglycate Disodium Cromoglycate (FPL 670, Cromolyn) 是一种抗过敏药,IC50为39 μg/mL。
S6994 TD-165 TD-165 是基于 PROTAC 技术的 CRBN 降解剂。 TD-165 包括一个 CRBN 配体结合基团,一个 linker 和一个 VHL 结合基团。
S5478 Dantrolene sodium Dantrolene sodium acts as a postsynaptic muscle relaxant by inhibiting Ca2+ ions release from sarcoplasmic reticulum stores by antagonizing ryanodine receptors.
Transl Stroke Res, 2022, 10.1007/s12975-022-01021-8
Oxid Med Cell Longev, 2021, 2021:8810698
Sci Rep, 2019, 9(1):3487
S1573 Fasudil (HA-1077) HCl Fasudil (HA-1077, AT-877)是一种有效的、具有选择性的Rho抑制剂(ROCK2, Ki=0.33 μM),同时对PKA、PKG、PKC和MLCK也具有抑制活性,Ki值分别为1.6 μM、1.6 μM、3.3 μM、36 μM。Fasudil 也是calcium channel的阻滞剂。
Aging Cell, 2022, e13587
Cell Death Dis, 2022, 13(2):138
iScience, 2022, 25(6):104398
S1356 Levetiracetam (UCB-L059) Levetiracetam (UCB-L059, SIB-S1) 是一种抗癫痫化合物。Levetiracetam (UCB-L059, SIB-S1) 是 muscarinic acetylcholine receptors (mAChR) 的激动剂并能调节突触前P/Q型压敏钙离子通道 calcium (Ca2+) channel
Anticancer Res, 2021, 41(2):687-697
PLoS One, 2019, 14(2):e0211644
Sci Rep, 2016, 6:25705
S1813 Amlodipine Besylate Amlodipine Besylate是一种长效的钙离子通道抑制剂,IC50为1.9 nM。
Cell Discov, 2020, 6(1):96
Oncogene, 2019, 38(1):120-139
S1293 Cilnidipine (FRC-8653) Cilnidipine (FRC-8653) 是一种L型和N型钙离子通道抑制剂,用来治疗高血压。
ACS Infect Dis, 2020, acsinfecdis.0c00486
Cell Discov, 2020, 6(1):96
Res Sq, 2020, rs.3.rs-48659
S1811 Amiloride (MK-870) HCl Amiloride (MK-870)是一种选择性的T-type calcium channel阻滞剂,epithelial sodium channel(ENaC)阻滞剂,urokinase plasminogen activator (uPA)抑制剂,Ki=7 μM。
Mol Ther Methods Clin Dev, 2022, 24:11-19
Adv Sci (Weinh), 2021, 8(13):2100962
Theranostics, 2021, 11(5):2364-2380
E0778New o-3M3FBS O-3M3FBS是m-3M3FBS的阴性对照,以独立于PLC的机制及拮抗的方式抑制内向和外向电流,可逆地抑制延迟整流K+通道,以与m-3M3FBS竞争的形式增加[Ca2+](i)
E0826New Levamlodipine Besylate Levamlodipine Besylate是一种强大的二氢吡啶钙通道(dihydropyridine calcium channel)阻滞剂,具有血管舒张特性,用于高血压和心绞痛的治疗。
S1425 Ranolazine 2HCl Ranolazine 2HCl (RS-43285)是一种钙离子通过 sodium/calcium channal摄取的抑制剂抗心绞痛药物,用于治疗慢性心绞痛。
Front Pharmacol, 2019, 10:1367
S4202 Verapamil (CP-16533-1) HCl Verapamil HCl (CP-16533-1)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
EMBO Mol Med, 2022, 14(2):e14903
Cell Rep, 2022, 38(10):110468
ACS Nano, 2021, 10.1021/acsnano.1c03517
S2482 Manidipine 2HCl Manidipine 2HCl (CV-4093) 是Manidipine的盐酸盐形式,是钙通道阻断剂,IC50为2.6 nM,临床上常用于抗高血压。Phase 4。
Environ Toxicol Chem, 2021, 10.1002/etc.5018
S1799 Ranolazine Ranolazine (CVT 303, RS 43285-003)是一种钙离子通过 sodium/calcium channal摄取的抑制剂抗心绞痛药物,用于治疗慢性心绞痛。
S1662 Isradipine Isradipine (PN 200-110)是一种高效选择性的L型压力控式钙离子通道抑制剂,用于治疗高血压。
Environ Toxicol Chem, 2021, 10.1002/etc.5018
Cell Discov, 2020, 6(1):96
Drug Metab Dispos, 2015, 43(12):1934-7
S1905 Amlodipine Amlodipine (UK-48340) 是一种长效的钙离子通道抑制剂,用于降低血压缓解胸部疼痛。
Oncogene, 2021, 40(6):1128-1146
ACS Infect Dis, 2020, acsinfecdis.0c00486
J Med Toxicol, 2020, 16(1):61-66
S1885 Felodipine Felodipine (CGH-869) 是一种选择性L型Ca2+通道阻断剂,IC50为0.15 nM。
ACS Infect Dis, 2020, acsinfecdis.0c00486
Cell Discov, 2020, 6(1):96
S2481 Manidipine Manidipine是一种二氢吡啶类钙拮抗剂,用于治疗高血压。
Antiviral Res, 2018, 150:130-136
S1748 Nisoldipine Nisoldipine (Sular, BAY K 5552)是特定L型CaV1.2钙通道阻断剂,IC50为10 nM。
Biomed Pharmacother, 2022, 145:112432
Cell Mol Gastroenterol Hepatol, 2021, S2352-345X(21)00196-X
Cell Discov, 2020, 6(1):96
S1747 Nimodipine Nimodipine (BAY E 9736) 是一种二氢吡啶衍生物,是钙离子通道抑制剂Nifedipine的类似物,具有降压活性。Nimodipine能减少细胞内游离Ca2+,Beclin-1及细胞自噬。
Cell Discov, 2020, 6(1):96
G3 (Bethesda), 2020, 4;10(5):1585-1597
Antiviral Res, 2016, 132:38-45
S2721 Nilvadipine Nilvadipine (ARC029, FR34235) 是一种强效钙通道阻滞剂,IC50为0.03 nM。
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Hum Cell, 2021, 10.1007/s13577-021-00639-4
Hum Cell, 2021, 34(6):1911-1918
S1994 Lacidipine Lacidipine (GX-1048, GR-43659X, SN-305)是一种L-型钙离子通道抑制剂。
S2114 Dronedarone HCl Dronedarone HCl (SR33589) 用于治疗阵发性和持续性房颤或房扑的患者。
Chem Res Toxicol, 2021, 10.1021/acs.chemrestox.1c00127
Cell Syst, 2019, 8(2):97-108
Nat Commun, 2016, 7:13023
S4181 Nicardipine HCl Nicardipine HCl (RS-69216)是二氢吡啶的钙通道抑制剂,具有显著的血管扩张作用。
ACS Infect Dis, 2020, acsinfecdis.0c00486
Cell Discov, 2020, 6(1):96
S1808 Nifedipine (BAY-a-1040) Nifedipine (BAY-a-1040)是一种二氢吡啶类钙离子通道阻滞剂,是有效的血管扩张剂,具有钙拮抗作用。
Oncogene, 2021, 40(6):1128-1146
Cell Discov, 2020, 6(1):96
Front Pharmacol, 2019, 10:381
S2080 Clevidipine Butyrate Clevidipine Butyrate是一种二氢吡啶类钙离子通道抑制剂,用于降血压。
ACS Infect Dis, 2020, acsinfecdis.0c00486
S2017 Benidipine HCl Benidipine HCl (KW-3049) 是Benidipine的盐酸盐形式,是一种二氢吡啶类的钙离子通道抑制剂。 
ACS Infect Dis, 2020, acsinfecdis.0c00486
Cell Discov, 2020, 6(1):96
Life Sci, 2019, 227:74-81
S2030 Flunarizine 2HCl Flunarizine 2HCl (KW-3149, R14950) 是一种二氢盐酸盐,抑制钙离子通道,Ki为68 nM。
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Hum Cell, 2021, 10.1007/s13577-021-00639-4
Hum Cell, 2021, 34(6):1911-1918
S2491 Nitrendipine Nitrendipine (Bayotensin) 是一种二氢吡啶类钙离子通道抑制剂,IC50为95 nM。
S3053 Azelnidipine Azelnidipine (UR-12592)是一种二氢吡啶类钙通道阻断剂。
Cell Mol Gastroenterol Hepatol, 2021, S2352-345X(21)00196-X
Environ Toxicol Chem, 2021, 10.1002/etc.5018
S2573 Tetracaine HCl Tetracaine HCl (Amethocalne)是Tetracaine的盐酸盐形式,是一种有效的局部麻醉剂和通道功能变构酶抑制剂。
S0000 Cav 2.2 blocker 1 Cav 2.2 blocker 1 (compound 9) 是一种 N-type calcium channel (Cav 2.2) 阻滞剂可用于治疗疼痛,其IC50值为0.001 μM。
S1865 Diltiazem HCl Diltiazem (Tiazac, RG 83606) HCl 是一种Benzothiazepine衍生物,具有舒张血管的作用,由于其抑制钙离子在膜的功能。
J Cell Mol Med, 2018, 22(12):5964-5977
FASEB J, 2017, 31(2):625-635
S3045 Cinepazide maleate Cinepazide maleate是cinepazide的马来酸盐形式,而cinepazide是一种血管舒张药。
S5255 Nicardipine Nicardipine is a potent calcium channel blockader with marked vasodilator action.
Cell Chem Biol, 2021, S2451-9456(21)00442-6
S3242 Loureirin B Loureirin B (LB, LrB),是从Dracaena cochinchinensis中提取的类黄酮,是 PAI-1 的抑制剂,其IC50值为26.10 μM。Loureirin B 可下调TGF-β1刺激的成纤维细胞中的 p-ERKp-JNK。Loureirin B 主要通过增加Pdx-1、MafA、细胞内ATP水平来促进胰岛素分泌,抑制 KATP 电流,Ca2+ 进入细胞内。
S8380 YM-58483 (BTP2) YM-58483/BTP2是钙池调控钙离子进入(SOCE)的阻滞剂,参与调解不可兴奋细胞如淋巴细胞的激活。
Dev Cell, 2022, S1534-5807(21)01035-2
Front Pharmacol, 2021, 12:622774
Cell Stem Cell, 2018, 22(6):865-878
S0535 FK962 FK962是FK960的衍生物,具有抗痴呆的特性,在1-1000 nM时,显著增强高K+诱导的大鼠海马片的生长抑素释放,在1-100 nM时,也显著降低生长抑素诱导的大鼠海马神经元的Ca2+通道抑制。
S6657 2-Aminoethyl Diphenylborinate (2-APB) 2-Aminoethyl Diphenylborinate (2-APB)是IP3 receptor的抑制剂,可以调节IP3诱导的钙释放。2-APB还可以抑制SOC通道的活性,并且在高浓度的时候可以激活TRP通道
Int J Biol Sci, 2021, 17(13):3672-3688
Int J Biol Sci, 2021, 17(13):3672-3688
Chem Biol Interact, 2021, 351:109756
S4626 Ethosuximide Ethosuximide是一种琥珀酰亚胺类的抗痉挛试剂,主要用于失神发作。是钙离子通道阻滞剂。
Nature, 2018, 554(7692):317-322
S5966 Amlodipine maleate Amlodipine (Amvaz, UK-48340) maleate 是一种长效的 calcium channel 的阻滞剂,可用于降低血压或预防胸痛。
S4597 Lercanidipine hydrochloride Lercanidipine是二氢吡啶类的钙离子通道抑制剂。
J Phys Chem B, 2013, 117(23):6868-73
S4977 Efonidipine Efonidipine (NZ-105) 是一种L型和T型钙离子通道阻滞剂,可引起血管舒张和心脏自律性降低。它还能抑制醛固酮从肾上腺分泌。
S5279 Fendiline hydrochloride Fendiline hydrochloride is the hydrochloride salt form of Fendiline, which is an L-type calcium channel blocker and also a specific inhibitor of K-Ras plasma membrane targeting with no detectable effect on the localization of H- and N-Ras.
S3845 Panaxadiol Panaxadiol (20(R)-Panaxadiol) is a triterpene sapogenin originally found in species of Panax (ginseng) and exhibits anticancer, cardioprotective, anti-arrhythmic, and antioxidative activities. It inhibits Ca2+ channels, decreasing channel open time and open state probability in vitro and displaying anti-arrhythmic potential.
S5898 Efonidipine hydrochloride monoethanolate Efonidipine (NZ-105) hydrochloride monoethanolate 是一种L型和T型 calcium channel 的阻滞剂,可导致血管舒张并降低心脏的自动节律性。Efonidipine hydrochloride monoethanolate 还抑制肾上腺醛固酮的分泌。
S3700 DHBP dibromide DHBP (1,1'-diheptyl-4,4'-bipyridinium),一种用于电致色记忆显示剂的紫罗碱,抑制由2 mM咖啡因和2 μg/ml多熔素诱导的钙释放,IC50分别为5 μg/ml和4 μg/ml。
S6834 CM 4620 CM 4620 是一种 calcium-release activated calcium-channel (CRAC channel) 的抑制剂。CM4620 抑制Orai1/STIM1介导的Ca2+电流和Orai2/STIM1介导的电流,对应的IC50值分别接近120 nM和900 nM。
S9017 Columbianadin Columbianadin (Zosimin, 2-Butenoic acid) 是一种来自当归的天然香豆素,已知具有多种生物活性,包括钙通道阻断活性、对各种癌细胞系的细胞毒活性、镇痛活性、肠道吸收和运输、抗炎和抗癌作用。
S2403 Tetrandrine (NSC-77037) Tetrandrine (NSC-77037, Fanchinine, d-Tetrandrine)是来源于千金藤根部的一种双苯基异喹啉,一种钙离子通道抑制剂。
FASEB J, 2021, 35(5):e21502
Nat Commun, 2020, 27;11(1):1620
Ann Transl Med, 2020, 8(16):1018
S9315 Praeruptorin A Praeruptorin A, a naturally existing pyranocumarin, is isolated from the dried root of Peucedanum praeruptorum Dunn. Praeruptorin A inhibits p38/Akt-c-Fos-NFATc1 signaling and PLCγ-independent Ca2+ oscillation. Praeruptorin A can significantly upregulates multidrug resistance-associated protein 2 expression via the constitutive androstane receptor-mediated pathway in vitro, and this should be taken as an herb-drug interaction.
S6920 SEA0400 SEA0400 是一种选择性的 Na+-Ca2+ exchanger (NCX) 的强效抑制剂,可抑制神经细胞、星形胶质细胞和小胶质细胞中Na+依赖性的Ca2+吸收,对应的IC50值分别为33 nM、5.0 nM和8.3 nM。SEA0400 可防止硝普钠 (SNP) 提高 ERKp38 MAPK 的磷酸化和通过细胞外Ca2+依赖的方式增强reactive oxygen species (ROS) 的产生。
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.
J Ethnopharmacol, 2021, S0378-8741(21)00169-0
S5514 Lanthanum(III) chloride heptahydrate Lanthanum(III) chloride is the inorganic compound used in biochemical research to block the activity of divalent cation channels, mainly calcium channels.
J Surg Res, 2021, 263:236-244
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).
S4084 Lomerizine 2HCl Lomerizine dihydrochloride (KB-2796) 是一种相对较新的L-和T-型钙通道阻滞剂,用于治疗偏头痛。
S4648 Dantrolene sodium hemiheptahydrate Dantrolene sodium hemiheptahydrate (Dantrium) 是一种骨骼肌松弛药,通过干扰肌纤维中的兴奋-收缩偶联起作用。
Cardiovasc Res, 2021, 117(4):1091-1102
Oxid Med Cell Longev, 2021, 2021:8810698
S3682 Ethyl 3-Aminobenzoate methanesulfonate Ethyl 3-Aminobenzoate (Ethyl m-Aminobenzoate, NSC 93790, Tricaine) 可通过voltage-dependent Na+-channels阻止动作电位的产生,常用于鱼类的麻醉、镇静和安乐死。
S9400 Rhynchophylline Rhynchophylline (Mitrinermine), an active component isolated from species of the genus Uncaria, acts as a calcium channel blocker and is widely used in traditional Chinese medicine mainly for treating ailments of central nervous and cardiovascular systems, such as lightheadedness, convulsions, numbness, and hypertension.
S3674 Levamlodipine Levamlodipine (S-amlodipine) is a pharmacologically active enantiomer of amlodipine which belongs to the dihydropyridine group of calcium channel blocker. It acts on the L-type of calcium channels and its treatment results in vasodilation and a fall in blood pressure.
Oncogene, 2021, 40(6):1128-1146
S3883 Protopine Protopine (Corydinine, Fumarine, Biflorine, Macleyine), an alkaloid present in different plants, has been shown to exhibit a number of activities, such as inhibition of calcium influx through both voltage and receptor-operated channels and inhibition of rabbit blood platelet aggregation. It also possesses anti-cholinergic and anti-histaminic as well as anti-bacterial activities.
S5567 Trimethadione Trimethadione is an oxazolidinedione anticonvulsant and often used to treat epileptic conditions that are resistant to other treatments.
S9566 Bepridil hydrochloride Bepridil hydrochloride是一种抗心绞痛的药物,是钙离子通道(calcium channel)阻滞剂。它能阻止多种其他离子通道,包括钠离子和钾离子通道。
S6847 ML-9 HCl ML-9 HCl (ML-9 hydrochloride) 是一种有效的选择性的 Akt kinasemyosin light chain kinase (MLCK)stromal interaction molecule 1 (STIM1)。ML-9 HCl 也是 Ca2+-permeable channels 的有效抑制剂。ML-9 HCl 是一种靶向自噬和细胞死亡的亲溶酶体剂。
J Mol Endocrinol, 2019, 63(3):199-213
S0452 NP118809 NP118809(39-1B4)是一种有效的N型钙通道(N-type calcium channel)阻滞剂,IC50为0.11 μM,对L型钙通道(L-type calcium channel)的抑制作用也较弱,IC50为12.2 μM。
S0016 SN-6 SN-6 是一种选择性的 Na+/Ca2+ exchanger (NCX) 抑制剂。SN-6 可抑制NCX1、NCX2和NCX3,对应的IC50值分别为2.9 μM、16 μM和8.6 μM。SN-6 可消除 acetylcholine (ACh) 诱导的血管舒张。
S6473 Pinaverium bromide Pinaverium bromide (Icosapentaenoic acid)是calcium channel阻滞剂,适用于治疗功能性胃肠病。
S4727 Cinnarizine Cinnarizine (Stugeron, Dimitronal, Stutgin, Cinarizine)是piperazine的药物衍生物,是抗组胺剂钙离子通道阻滞剂。
S9842 MCU-i4 MCU-i4 是 mitochondrial calcium uniporter (MCU) 复合物的负调节剂,可直接结合 MICU1 中的特定裂缝并减少线粒体 Ca2+ 流入。
S2050 Strontium Ranelate Strontium Ranelate 是Ranelic acid的锶(II)盐,用于(-)-Desmethoxyverapamil结合到钙离子通道,IC50为0.5 mM。
S7924 Bay K 8644 Bay K 8644是一种高选择性的L型钙离子通道激动剂,EC50为17.3 nM。
ACS Nano, 2021, 10.1021/acsnano.1c03517
Cell Biol Toxicol, 2021, 10.1007/s10565-021-09615-y
Journal of Advanced Research, 2020, 10.1016/j.jare.2020.10.005
S4209 Chlorocresol Chlorocresol 是ryanodine receptor激活剂。
E0777New Z944 Z944是一种高度选择性的T型钙通道拮抗剂,对hCaV3.1、hCaV3.2和hCaV3.3的IC50分别为50、160、110 nM。
E0945New BIA BIA (TMBIM6 antagonist BIA)是一个潜在的TMBIM6拮抗剂,可以阻断TMBIM6和mTORC2的相互作用,最终阻断AKT的激活和癌症进展。
S4931 Propiverine hydrochloride Propiverine是一种抗胆碱能药物,用于治疗膀胱过度活动症和尿失禁。
S0870 Barnidipine Barnidipine (Libradin, Mepirodipine, Vasexten, YM-09730-5, Cyress, Hypoca, Oldeca) 是一种降压药,属于dihydropyridine (DHP)组的calcium 拮抗剂 (CaA),对[3H]nitrendipine 结合位点的Ki值为0.21 nM。
S3809 Imperatorin Imperatorin (Ammidin, Marmelosin, Pentosalen, 8-Isoamylenoxypsoralen), a naturally occurring psoralen-type furanocoumarin, is a potent myorelaxant agent and acts as a calcium antagonist on vascular smooth muscle.
Front Cell Dev Biol, 2020, 8:592433
Adv Sci (Weinh), 2020, 7(16):2000925
Theriogenology, 2019, 10.1016/j.theriogenology
S2436 Pranidipine Pranidipine (Acalas, OPC 13340)是一种新型的1,4-二氢吡啶 calcium channel 阻滞剂。Pranidipine可以增强cyclic GMP依赖性一氧化氮诱导的大鼠主动脉舒张。
S5861 Lercanidipine Lercanidipine是一种对血管具有特异性的钙离子通道拮抗剂,可用于治疗发性高血压。
E0137New GV-58 GV-58 是一种新型的选择性 N 型和 P/Q 型 Ca2+ 通道激动剂,IC50 分别为 7.21 μM 和 8.81 μM。
S5191 Cinacalcet Cinacalcet (AMG073, Sensipar, Cin) 是一种口服活性的 receptors for calcium (CaR) 的变构激动剂,可增加CaR对Ca的敏感性。
Int J Mol Sci, 2022, 23(8)4323
S9151 Praeruptorin E Praeruptorin E, isolated from Peucedanum praeruptorum Dunn., is a cardiotonic agent with selective cardiac calcium channel agonistic effect.
E0936New IGS-1.76 IGS-1.76是一种蛋白-蛋白相互作用(protein-protein interaction, PPI)抑制剂,具有药物样特性,对人类神经钙传感蛋白1(human neuronal calcium sensor 1, hNCS-1)具有显著的亲和力,并有效地调节hNCS-1和鸟嘌呤交换因子Ric8a的相互作用。
S2535 Econazole nitrate Econazole Nitrate (NSC 243115) 是一种咪唑类抗真菌药物。
Biomol Ther (Seoul), 2020, 25
S0713 S107 hydrochloride S107 hydrochloride 是一种 RyR2 (type 2 ryanodine receptor)/FKBP12.6 (FK506 binding protein 12.6) complex 的特异性稳定剂,会影响 Ca2+ 信号传导。
S3236 Mesaconitine Mesaconitine 是Aconiti tuber附子块茎中的附子生物碱之一,通过从细胞外空间流入Ca2+来增加内皮细胞中的[Ca2+]i水平。
S0973 Wilforgine Wilforgine 是 Tripterygium wilfordii Hook. F.中主要的生物活性倍半萜生物碱之一,可在M. separata larvae的肌肉中诱导显微结构和超微结构变化,其发挥作用的位置是肌肉系统中的 calcium receptors or channels
S2415 Astragaloside A Astragaloside A是从黄芪中分离的一种纯化的皂苷,广泛应用于治疗心血管疾病。
Sci Rep, 2022, 12(1):7
Carcinogenesis, 2020, 41(7):993-1004
J Med Virol, 2019, 91(8):1440-1447
S3191 Azumolene Azumolene(EU4093 free base)是一种等效的丹曲林(dantrolene)类似物,是一种兰尼碱受体 (ryanodine receptor, RyR) 调节剂,可抑制钙释放。
S4353 Terfenadine Terfenadine is an antihistamine, generally completely metabolizes to the active form fexofenadine in the liver by the enzyme cytochrome P450 CYP3A4 isoform. Terfenadine ((±)-Terfenadine) is a potent open-channel blocker of hERG with an IC50 of 204 nM. Terfenadine, an H1 histamine receptor antagonist, acts as a potent apoptosis inducer in melanoma cells through modulation of Ca2+ homeostasis. Terfenadine induces ROS-dependent apoptosis, simultaneously activates Caspase-4, -2, -9.
E0778New o-3M3FBS O-3M3FBS是m-3M3FBS的阴性对照,以独立于PLC的机制及拮抗的方式抑制内向和外向电流,可逆地抑制延迟整流K+通道,以与m-3M3FBS竞争的形式增加[Ca2+](i)
E0826New Levamlodipine Besylate Levamlodipine Besylate是一种强大的二氢吡啶钙通道(dihydropyridine calcium channel)阻滞剂,具有血管舒张特性,用于高血压和心绞痛的治疗。
E0777New Z944 Z944是一种高度选择性的T型钙通道拮抗剂,对hCaV3.1、hCaV3.2和hCaV3.3的IC50分别为50、160、110 nM。
E0945New BIA BIA (TMBIM6 antagonist BIA)是一个潜在的TMBIM6拮抗剂,可以阻断TMBIM6和mTORC2的相互作用,最终阻断AKT的激活和癌症进展。
E0137New GV-58 GV-58 是一种新型的选择性 N 型和 P/Q 型 Ca2+ 通道激动剂,IC50 分别为 7.21 μM 和 8.81 μM。
E0936New IGS-1.76 IGS-1.76是一种蛋白-蛋白相互作用(protein-protein interaction, PPI)抑制剂,具有药物样特性,对人类神经钙传感蛋白1(human neuronal calcium sensor 1, hNCS-1)具有显著的亲和力,并有效地调节hNCS-1和鸟嘌呤交换因子Ric8a的相互作用。
Tags: Calcium Channel inhibitor|Calcium Channel agonist|Calcium Channel activator|Calcium Channel inducer|Calcium Channel antagonist|Calcium Channel signaling pathway|Calcium Channel assay kit