Clopidogrel hydrogen sulfate

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Chemical Structure| 120202-66-6 同义名 : (S)-(+)-氯吡格雷硫酸盐 ;(S)-(+)-Clopidogrel hydrogen sulfate;(S)-(+)-Clopidogrel bisulfate;SR 25990C;(S)-(+)-Clopidogrel (sulfate);Clopidogrel Bisulfate
CAS号 : 120202-66-6
货号 : A749538
分子式 : C16H18ClNO6S2
纯度 : 98%
分子量 : 419.9
MDL号 : MFCD00876395
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 45 mg/mL(107.17 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 15 mg/mL(35.72 mM)，配合低频超声助溶
动物实验配方：
生物活性
靶点

  • P2Y receptor
描述 Clopidogrel hydrogen sulfate is an antiplatelet agent which works by blocking platelets from sticking together and prevents them from forming harmful clots. Clopidogrel abolishes the inhibitory P2Y(AC) receptor-mediated ADP effects on prostaglandin E(1)-stimulated, cAMP-dependent phosphorylation of VASP (vasodilator-stimulated phosphoprotein) without affecting epinephrine, thrombin, and thromboxane signaling[3]. The inhibitory effect of clopidogrel on platelet consumption by the growing thrombi resulted apparently in higher platelet concentration at the collagen surface, which enhanced the platelet-collagen adhesion at all three shear rates[4]. Clopidogrel therapy resulted in a significant reduction in soluble CD40 ligand (P = 0.03), a prothrombotic and proinflammatory molecule derived mainly from activated platelets[5]. Clopidogrel (clopi) is a prodrug widely prescribed in the management of coronary artery disease and requires the intervention of hepatic cytochrome P450 2C19 (CYP2C19) for its activation[6]. Resistance to clopidogrel is largely a result of CYP2C19 enzyme loss of function alleles. One-year patency rates following lower extremity arterial endovascular interventions in patients with clopidogrel resistance (HPR) range between 35%-83% whereas those with the proper response to clopidogrel range between 73%-100%[7].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.38mL

0.48mL

0.24mL

11.91mL

2.38mL

1.19mL

23.82mL

4.76mL

2.38mL
参考文献

[1]Luo JC, Huo TI, et al. Clopidogrel delays gastric ulcer healing in rats. Eur J Pharmacol. 2012 Nov 15;695(1-3):112-9.

[2]Laine L, Hennekens C. Proton pump inhibitor and clopidogrel interaction: fact or fiction? Am J Gastroenterol. 2010 Jan;105(1):34-41.

[3]Geiger J, Brich J, Hönig-Liedl P, Eigenthaler M, Schanzenbächer P, Herbert JM, Walter U. Specific impairment of human platelet P2Y(AC) ADP receptor-mediated signaling by the antiplatelet drug clopidogrel. Arterioscler Thromb Vasc Biol. 1999 Aug;19(8):2007-11

[4]Roald HE, Barstad RM, Kierulf P, Skjørten F, Dickinson JP, Kieffer G, Sakariassen KS. Clopidogrel--a platelet inhibitor which inhibits thrombogenesis in non-anticoagulated human blood independently of the blood flow conditions. Thromb Haemost. 1994 May;71(5):655-62

[5]Ramadan R, Dhawan SS, Syed H, Pohlel FK, Binongo JN, Ghazzal ZB, Quyyumi AA. Effects of clopidogrel therapy on oxidative stress, inflammation, vascular function, and progenitor cells in stable coronary artery disease. J Cardiovasc Pharmacol. 2014 Apr;63(4):369-74

[6]Charfi R, Mzoughi K, Boughalleb M, Hosni H, Kouidhi S, Sfar I, Hammami N, Zaïri I, Limam M, Zedini C, Mrabet A, Klouz A, Gorgi Y, Kharrat M, Baccar H, Trabelsi S. Response to clopidogrel and of the cytochrome CYP2C19 gene polymorphism. Tunis Med. 2018 Mar;96(3):209-218

[7]Markel KM, Avgerinos ED. Clopidogrel Resistance in Lower Extremity Arterial Endovascular Interventions. Curr Pharm Des. 2018;24(38):4554-4557