Clopidogrel hydrogen sulfate

Clopidogrel hydrogen sulfate是一种通过抑制CYP2B6和CYP2C19防止血栓形成的抗血小板药物，IC50分别为18.2 nM和524 nM。它是一种高效的抗血栓药物，抑制ADP诱导的血小板聚集，也是口服活性的P2Y(12)抑制剂。

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 signaling³. 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 rates⁴. Clopidogrel therapy resulted in a significant reduction in soluble CD40 ligand (P = 0.03), a prothrombotic and proinflammatory molecule derived mainly from activated platelets⁵. 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 activation⁶. 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.

溶解方案(细胞实验)

DMSO 中的溶解度 : ≥ 46.7 mg/mL (111.22 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)|H₂O 中的溶解度 : 16.67 mg/mL (39.70 mM; 超声助溶)|* "≥" means soluble, but saturation unknown.

溶解方案(动物实验)

"方案 一": "请依序添加每种溶剂：10% DMSO 90% (20% SBE-β-CD in Saline)Solubility: ≥ 2.08 mg/mL (4.95 mM); 澄清溶液 此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。"

"方案 二": "请依序添加每种溶剂：10% DMSO 90% Corn OilSolubility: ≥ 2.08 mg/mL (4.95 mM); 澄清溶液 此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。"

"方案 一": "请依序添加每种溶剂：PBSSolubility: 50 mg/mL (119.08 mM); 澄清溶液; 超声助溶"