CAS 159138-80-4|Cariporide

Introduction：Basic information about CAS 159138-80-4|Cariporide, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. Cariporide BiologicalActivity
3. Chemical & Physical Properties
4. Safety Information
5. Synonyms

Common Name	Cariporide
CAS Number	159138-80-4	Molecular Weight	283.347
Density	1.3±0.1 g/cm3	Boiling Point	542.8±60.0 °C at 760 mmHg
Molecular Formula	C₁₂H₁₇N₃O₃S	Melting Point	/
MSDS	ChineseUSA	Flash Point	282.1±32.9 °C

Names

Name	N-(diaminomethylidene)-3-methylsulfonyl-4-propan-2-ylbenzamide
Synonym	More Synonyms

Cariporide BiologicalActivity

Description	Cariporide (HOE-642) is a selective Na+/H+ exchange inhibitor.
Related Catalog	Signaling Pathways >>Membrane Transporter/Ion Channel >>Sodium ChannelResearch Areas >>Cardiovascular DiseaseResearch Areas >>Inflammation/Immunology
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].
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].
Animal Admin	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].
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. [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. [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.

Chemical & Physical Properties

Density	1.3±0.1 g/cm3
Boiling Point	542.8±60.0 °C at 760 mmHg
Molecular Formula	C₁₂H₁₇N₃O₃S
Molecular Weight	283.347
Flash Point	282.1±32.9 °C
Exact Mass	283.099060
PSA	123.99000
LogP	0.40
Vapour Pressure	0.0±1.4 mmHg at 25°C
Index of Refraction	1.602
InChIKey	IWXNYAIICFKCTM-UHFFFAOYSA-N
SMILES	CC(C)c1ccc(C(=O)N=C(N)N)cc1S(C)(=O)=O
Storage condition	2-8℃

Safety Information

RIDADR	NONH for all modes of transport
RTECS	CV2310560

Synonyms

HOE642

Cariporide

N-(Diaminomethylene)-4-isopropyl-3-(methylsulfonyl)benzamide

Benzamide, N-(diaminomethylene)-4-(1-methylethyl)-3-(methylsulfonyl)-

N-Carbamimidoyl-4-isopropyl-3-(methylsulfonyl)benzamide

benzamide, N-(aminoiminomethyl)-4-(1-methylethyl)-3-(methylsulfonyl)-

N-(diaminomethylidene)-3-(methylsulfonyl)-4-(propan-2-yl)benzamide

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