KB-R7943 mesylate|cas 182004-65-5|DC Chemicals

Cas No.:	182004-65-5
Chemical Name:	KB-R7943 mesylate
Synonyms:	2-[2-[4-(4-NITROBENZYLOXY)PHENYL]ETHYL]ISOTHIOUREA MESYLATE;S-[4-[(4-Nitrobenzyl)oxy]phenethyl]isothiourea Methanesulfonate;4-((4-Nitrobenzyl)oxy)phenethyl carbamimidothioate methanesulfonate;KB-R7943;KB-R7943 (mesylate);KB-R7943 MESYLATE;KB-R7943 MESYLATE KB-R7943;KB-R7943 MESYLATE KB-R7943;methanesulfonic acid,2-[4-[(4-nitrophenyl)methoxy]phenyl]ethyl carbamimidothioate;4-[(4-Nitrobenzyl)oxy]phenethyl Carbamimidothioate Methanesulfonate;Carbamimidothioic Acid 4-[(4-Nitrobenzyl)oxy]phenethyl Ester Methanesulfonate;HMS3267H09;Carbamimidothioic acid 2-[4-[(4-nitrophenyl)methoxy]phenyl]ethyl ester methanesulfonate;Carbamimidothioic acid 2-[4-[(4-nitrophenyl)methoxy]phenyl]ethyl ester monomethanesulfonate;2-(2-(4-(4-NITROBENZYLOXY)PHENYL)ETHYL)ISOTHIOUREA, METHANE SULFONATE;KB-R 7943;4-((4-Nitrobenzyl)oxy)phenethyl carbamimidothioatemethanesulfonate;GTPL4232;CT
SMILES:	N=C(N)SCCC1=CC=C(OCC2=CC=C([N+]([O-])=O)C=C2)C=C1.OS(=O)(C)=O
Formula:	C₁₇H₂₁N₃O₆S₂
M.Wt:	427.49
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

KB-R7943 mesylate is a widely used inhibitor of the reverse Na+/Ca2+ exchanger (NCXrev) with IC50 of 5.7±2.1 µM.

In Vitro:

KB-R7943 mesylate blocks NMDAR-mediated ion currents, and inhibits NMDA-induced increase in cytosolic Ca2+ with IC50=13.4±3.6 µM but accelerates calcium deregulation and mitochondrial depolarization in glutamate-treated neurons. KB-R7943 depolarizes mitochondria in a Ca2+-independent manner. KB-R7943 inhibits 2,4-dinitrophenol-stimulated respiration of cultured neurons with IC50=11.4±2.4 µM. In addition to NCXrev, KB-R7943 dose-dependently and reversibly blocked ion currents elicited by NMDA. KB-R7943 dose-dependently inhibits NMDA-induced increases in [Ca2+]c with IC50=13.4±3.6 µM confirming the inhibition of NMDA receptors observed in electrophysiological experiments[1]. wtRyR1-HEK 293 pretreated with KB-R7943 (10 μM, 10 min) dissolved in the bulk perfusion exhibited significantly attenuated responses to caffeine. In this regard, KB-R7943 produced more pronounced inhibition of caffeine-induced Ca2+ release elicited by 1 mM compared with 0.5 and 0.75 mM (60 versus 58 versus 37%, p<0.05, respectively)[2]. KB-R7943 inhibits both IhERG and native IKr rapidly on membrane depolarization with IC50 values of ~89 and ~120 nM, respectively, for current tails at −40 mV following depolarizing voltage commands to +20 mV. IhERG inhibition by KB-R7943 exhibits both time- and voltage-dependence but shows no preference for inactivated over activated channels[3].

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