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Clopidogrel hydrogen sulfate/硫酸氢氯吡格雷 {[allProObj[0].p_purity_real_show]}

货号:A749538 同义名: (S)-(+)-氯吡格雷硫酸盐 / (S)-(+)-Clopidogrel hydrogen sulfate; (S)-(+)-Clopidogrel bisulfate

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。

HazMat Fee +

There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Clopidogrel hydrogen sulfate/硫酸氢氯吡格雷 化学结构 CAS号:120202-66-6
Clopidogrel hydrogen sulfate/硫酸氢氯吡格雷 化学结构
CAS号:120202-66-6
Clopidogrel hydrogen sulfate/硫酸氢氯吡格雷 3D分子结构
CAS号:120202-66-6
Clopidogrel hydrogen sulfate/硫酸氢氯吡格雷 化学结构 CAS号:120202-66-6
Clopidogrel hydrogen sulfate/硫酸氢氯吡格雷 3D分子结构 CAS号:120202-66-6
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Clopidogrel hydrogen sulfate/硫酸氢氯吡格雷 纯度/质量文件 产品仅供科研

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Clopidogrel hydrogen sulfate/硫酸氢氯吡格雷 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].

Clopidogrel hydrogen sulfate/硫酸氢氯吡格雷 细胞实验

Cell Line
Concentration Treated Time Description References
Bone marrow-derived macrophages (BMDMs) 5 ng/mL 5 days To investigate the induction of P2Y12 expression by TGF-β1 in BMDMs, the results showed that TGF-β1 induced P2Y12 expression via a Smad3-dependent mechanism, and inhibition of P2Y12 could block MMT and collagen matrix production. Mol Ther. 2022 Sep 7;30(9):3017-3033.

Clopidogrel hydrogen sulfate/硫酸氢氯吡格雷 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Mice Photothrombotic stroke model Intraperitoneal injection 40 mg/kg Daily for 14 days To evaluate the impact of clopidogrel on cognitive and motor function recovery post-stroke in mice. Results showed that clopidogrel significantly impaired learning and memory recovery, reduced mouse survival rates, and decreased body weight. Additionally, clopidogrel significantly increased vascular leakage, increased the number and altered the morphology of microglia, and reduced the number of T cells in the peri-infarct region post-stroke. Int J Mol Sci. 2023 Jul 20;24(14):11706
C57BL/6J and IL-1R−/− mice Diet-induced obesity model Oral 5 mg/kg Single dose To study the responsiveness of clopidogrel in diet-induced obese mice, results showed that wild-type DIO mice exhibited resistance to the anti-platelet and anti-thrombotic effects of clopidogrel, while IL-1R?/? DIO mice showed no resistance. Arterioscler Thromb Vasc Biol. 2020 Jun;40(6):1533-1542
LysM-Cre/Rosa26-tdTomato mice Unilateral ureteral obstruction (UUO) model Oral 60 mg/kg/day Once daily for 7 days To investigate the inhibitory effect of clopidogrel on renal fibrosis in UUO mice, the results showed that clopidogrel significantly inhibited renal fibrosis, P2Y12 expression, and TGF-β/Smad3 signaling pathway. Mol Ther. 2022 Sep 7;30(9):3017-3033.

Clopidogrel hydrogen sulfate/硫酸氢氯吡格雷 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

Clopidogrel hydrogen sulfate/硫酸氢氯吡格雷 实验方案

计算器
存储液制备 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

Clopidogrel hydrogen sulfate/硫酸氢氯吡格雷 技术信息

CAS号120202-66-6
分子式C16H18ClNO6S2
分子量 419.9
SMILES Code ClC1=C([C@@H](C(OC)=O)N2CCC3=C(C=CS3)C2)C=CC=C1.O=S(O)(O)=O
MDL No. MFCD00876395
别名 (S)-(+)-氯吡格雷硫酸盐 ;(S)-(+)-Clopidogrel hydrogen sulfate; (S)-(+)-Clopidogrel bisulfate; SR 25990C; (S)-(+)-Clopidogrel (sulfate); Clopidogrel Bisulfate
运输蓝冰
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Inert atmosphere, 2-8°C

溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案 一
方案 二
配制的工作液建议现用现配,短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案 一
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