KB-R7943 MESYLATE | CAS 182004-65-5

Element: mesylate r7943

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C-S » Chemicals » mesylate-PX82163

Identification

KB-R7943 MESYLATE

CAS:

182004-65-5

EINECS:

Molecular Formula:

C₁₆H₁₇N₃O₃S.CH₃SO₃H

MDL:

MFCD00952138

SMILES:

CS(=O)(=O)O.C1=CC(=CC=C1CCSC(=N)N)OCC2=CC=C(C=C2)[N+](=O)[O-]

Synonym:

2-[2-[4-(4-nitrobenzyloxy)phenyl]ethyl]isothiourea mesylate ; kb-r7943 ; kb-r7943 mesylate ; carbamimidothioic acid 2-[4-[(4-nitrophenyl)methoxy]phenyl]ethyl ester methanesulfonate ; carbamimidothioic acid 2-[4-[(4-nitrophenyl)methoxy]phenyl]ethyl ester monomethanesulfonate ; 4-((4-nitrobenzyl)oxy)phenethyl carbamimidothioate methanesulfonate ; s-[4-[(4-nitrobenzyl)oxy]phenethyl]isothiourea methanesulfonate ; 2-(2-(4-(4-nitrobenzyloxy)phenyl)ethyl)isothiourea, methane sulfonate

Description

KB-R7943 mesylate is a cell permeable, potent, selective NCKX inhibitor of the reverse mode of Na⁺/Ca²⁺ exchange in cells expressing NCX1. NCX1 is a Na⁺/Ca²⁺ exchanger predominantly expressed in cardiac sarcolemma, as well as in brain, kidney, liver, pancreas, skeletal muscle, placenta and lung. NCX1 expression is up-regualted in human heart failure, as well as in other animal heart failure models. KB-R7943 reversibly inhibits inward and outward Na⁺/Ca²⁺ exchange in a dose-dependent manner, although it inhibits outward exchange more potently. Non-competitive with respect to Na⁺/Ca²⁺ and exhibits neuroprotection against glutamate excitotoxicity in rat cultured cerebellar granule neurons. KB-R7943 suppressed ventricular arrhythmias (tachycardia and fibrillation) associated with both ischemia and reperfusion almost completely in a rabbit ischemia-reperfusion model of cardiac injury. KB-R7943 is also a potent blocker of the transient receptor potential channels (TRPC) TRPC3, TRPC5 and TRPC6. KB-R7943 MESYLATE is an inhibitor of NCX1, NCX2, NCX3 and CCDC109.

Suppliers

CSNpharm, Inc.

CSN12367

Leap Chem Co., Ltd

LC6121836

Santa Cruz Biotechnology, Inc.

202681

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