Cariporide

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Chemical Structure| 159138-80-4 同义名 : HOE-642 Free Base;HOE 642
CAS号 : 159138-80-4
货号 : A217757
分子式 : C12H17N3O3S
纯度 : 99%+
分子量 : 283.347
MDL号 : MFCD00864683
存储条件：

Pure form Keep in dark place,Sealed in dry,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(370.57 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
动物实验配方：
生物活性
描述 Cariporide remarkably suppressed cytosolic Na+ and Ca2+ accumulation. Mitochondrial Ca2+ overload induced by H2O2 was remarkably suppressed by cariporide. Cariporide prevented mitochondrial membrane potential loss induced by H2O2. Cariporide protects cardiomyocytes against oxidant-induced cell death by preserving intracellular ion homeostasis and mitochondrial integrity[3]. Cariporide (HOE-642) ameliorates myocardial ischemia/reperfusion injury, by the well-established reduction of cytosolic Ca2+ in cardiac myocytes through inhibition of Na+/H+ exchange[4]. Cariporide might inhibit HG-mediated monocyte-endothelial cell adhesion and expression of ICAM-1 (intercellular adhesion molecule-1) by inhibiting the activation of NHE-1(Na(+)/H(+) exchanger 1)[5]. Moreover, cariporide significantly facilitates the sensitivity of breast cancer to doxorubicin both in vitro and in vivo[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.53mL

0.71mL

0.35mL

17.65mL

3.53mL

1.76mL

35.29mL

7.06mL

3.53mL
参考文献

[1]Chakrabarti S, Hoque AN, Karmazyn M. A rapid ischemia-induced apoptosis in isolated rat hearts and its attenuation by the sodium-hydrogen exchange inhibitor HOE 642 (cariporide). J Mol Cell Cardiol. 1997 Nov;29(11):3169-74.

[2]Scholz W, Albus U, et al. Protective effects of HOE642, a selective sodium-hydrogen exchange subtype 1 inhibitor, on cardiac ischaemia and reperfusion. Cardiovasc Res. 1995 Feb;29(2):260-8.

[3]Teshima Y, Akao M, Jones SP, Marbán E. Cariporide (HOE642), a selective Na+-H+ exchange inhibitor, inhibits the mitochondrial death pathway. Circulation. 2003 Nov 4;108(18):2275-81

[4]Chang HB, Gao X, Nepomuceno R, Hu S, Sun D. Na(+)/H(+) exchanger in the regulation of platelet activation and paradoxical effects of cariporide. Exp Neurol. 2015 Oct;272:11-6

[5]Wang SX, Sun XY, Zhang XH, Chen SX, Liu YH, Liu LY. Cariporide inhibits high glucose-mediated adhesion of monocyte-endothelial cell and expression of intercellular adhesion molecule-1. Life Sci. 2006 Aug 29;79(14):1399-404

[6]Chen Q, Liu Y, Zhu XL, Feng F, Yang H, Xu W. Increased NHE1 expression is targeted by specific inhibitor cariporide to sensitize resistant breast cancer cells to doxorubicin in vitro and in vivo. BMC Cancer. 2019 Mar 8;19(1):211