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Cariporide

MCE China：Cariporide

Brand：MedChemExpress (MCE)

Cat. No.HY-19693

CAS：159138-80-4

Synonyms：HOE-642 Free Base

Purity：99.89%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Cariporide (HOE-642) is a selective Na+/H+ exchange inhibitor.

In Vitro：Cariporide significantly suppresses markers of cell death, such as TUNEL positivity and caspase-3 cleavage, at 8 or 16 hours. Cariporide remarkably suppresses cytosolic Na+ and Ca2+ accumulation. Cariporide prevents mitochondrial membrane potential loss induced by H2+O2+[1]. 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[2]. Cariporide (HOE-642), has inhibitory effects on the degranulation of human platelets, the formation of platelet–leukocyte-aggregates, and the activation of the GPIIb/IIIa receptor (PAC-1)[3].

In Vivo：Intravenous administration of cariporide significantly decreases brain Na+ uptake and reduces cerebral edema, brain swelling, and infarct volume[4].

Animal Administration：Rats: Cariporide and/or bumetanide are administered intravenously (15 or 30 mg/kg in 2 to 4 doses, respectively, of 7.5 mg/kg) starting at 20 minutes before initiation of pMCAO. For neurologic outcome experiments, some rats are given cariporide and/or bumetanide by a single intraperitoneal injection[4].

Cell Assay：Neonatal rat cardiomyocytes are randomly separated into groups: (1) control group, (2) incubation with 100 μM hydrogen peroxide, or (3) pretreatment with 10 μM cariporide for 20 minutes followed by 100 μM hydrogen peroxide. Caspase-3 activity is measured by detection of the cleavage of a colorimetric caspase-3 substrate, N-acetyl-Asp-Glu-Val-Asp-p-nitroaniline, using an assay kit[1].

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References：

[1]. Teshima Y, et al. Cariporide (HOE642), a selective Na+-H+ exchange inhibitor, inhibits the mitochondrial death pathway. Circulation. 2003 Nov 4;108(18):2275-81.  [Content Brief]

[2]. Chang HB, et al. Na(+)/H(+) exchanger in the regulation of platelet activation and paradoxical effects of cariporide. Exp Neurol. 2015 Oct;272:11-6.  [Content Brief]

[3]. O'Donnell ME, et al. Intravenous HOE-642 reduces brain edema and Na uptake in the rat permanent middle cerebral artery occlusion model of stroke: evidence for participation of the blood-brain barrier Na/H exchanger. J Cereb Blood Flow Metab. 2013 Feb;33(2):225-34.