CAS 182004-65-5|KB-R7943 mesylate
Introduction：Basic information about CAS 182004-65-5|KB-R7943 mesylate, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
| Common Name | KB-R7943 mesylate | ||
|---|---|---|---|
| CAS Number | 182004-65-5 | Molecular Weight | 427.495 |
| Density | / | Boiling Point | 534.6ºC at 760mmHg |
| Molecular Formula | C17H21N3O6S2 | Melting Point | / |
| MSDS | ChineseUSA | Flash Point | 277.1ºC |
Names
| Name | methanesulfonic acid,2-[4-[(4-nitrophenyl)methoxy]phenyl]ethyl carbamimidothioate |
|---|---|
| Synonym | More Synonyms |
KB-R7943 mesylate BiologicalActivity
| Description | KB-R7943 mesylate is a widely used inhibitor of the reverse Na+/Ca2+ exchanger (NCXrev) with IC50 of 5.7±2.1 µM. |
|---|---|
| Related Catalog | Signaling Pathways >>Membrane Transporter/Ion Channel >>Na+/Ca2+ ExchangerResearch Areas >>Others |
| Target | IC50: 5.7±2.1 µM (Na+/Ca2+ exchanger)[1] |
| 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]. |
| Cell Assay | EK 293 cells stably expressing the wtRyR1 (wtRyR1-HEK 293) are maintained in Dulbecco's modified Eagle's medium supplemented with 2 mM glutamine, 100 μg/mL streptomycin, 100 U/mL penicillin, 1 mM sodium pyruvate, and 10% fetal bovine serum at 37°C under 5% CO2. wtRyR1-HEK 293 cells are loaded with 5 μM Fluo-4 acetoxymethyl ester at 37°C for 30 min to measure Ca2+ transients in an imaging buffer consisting of 140 mM NaCl, 5 mM KCl, 2 mM MgCl2, 2 mM CaCl2, 10 mM HEPES, and 10 mM glucose, pH 7.4, supplemented with 0.05% bovine serum albumin. The cells are washed three times with imaging buffer and additionally incubated for 20 min at room temperature. Dye-loaded cells are washed three times with imaging buffer and imaged with a charge-coupled device camera with a 40× objective lens attached to an IX-71 microscope. The sequence of images is captured and monitored using EasyRatioPro. Caffeine dissolved in the imaging buffer is focally applied for 15 s using AutoMate Scientific. KB-R7943 is dissolved in the imaging buffer, and wtRyR1-HEK 293 cells are incubated for 10 min before the application of caffeine[2]. |
| References | [1]. Brustovetsky T, et al. KB-R7943, an inhibitor of the reverse Na+ /Ca2+ exchanger, blocks N-methyl-D-aspartate receptor and inhibits mitochondrial complex I. Br J Pharmacol. 2011 Jan;162(1):255-70. [2]. Barrientos G, et al. The Na+/Ca2+ exchange inhibitor 2-(2-(4-(4-nitrobenzyloxy)phenyl)ethyl)isothiourea methanesulfonate(KB-R7943) also blocks ryanodine receptors type 1 (RyR1) and type 2 (RyR2) channels. Mol Pharmacol. 2009 Sep;76(3):560-8. [3]. Cheng H, et al. High potency inhibition of hERG potassium channels by the sodium-calcium exchange inhibitor KB-R7943. Br J Pharmacol. 2012 Apr;165(7):2260-73. |
Chemical & Physical Properties
| Boiling Point | 534.6ºC at 760mmHg |
|---|---|
| Molecular Formula | C17H21N3O6S2 |
| Molecular Weight | 427.495 |
| Flash Point | 277.1ºC |
| Exact Mass | 427.087189 |
| PSA | 192.97000 |
| LogP | 5.25100 |
| Vapour Pressure | 1.67E-11mmHg at 25°C |
| InChIKey | WGIKEBHIKKWJLG-UHFFFAOYSA-N |
| SMILES | CS(=O)(=O)O.N=C(N)SCCc1ccc(OCc2ccc([N+](=O)[O-])cc2)cc1 |
| Storage condition | 2-8°C |
Synonyms
| HMS3267H09 |
| KB-R7943 mesylate |
| KB-R7943 |
| MFCD00237019 |
| 2-{4-[(4-Nitrobenzyl)oxy]phenyl}ethyl carbamimidothioate methanesulfonate (1:1) |
| Carbamimidothioic Acid 4-[(4-Nitrobenzyl)oxy]phenethyl Ester Methanesulfonate |
| 4-[(4-Nitrobenzyl)oxy]phenethyl Carbamimidothioate Methanesulfonate |
| Carbamimidothioic acid, 2-[4-[(4-nitrophenyl)methoxy]phenyl]ethyl ester, methanesulfonate (1:1) |
| KB-R7943 (mesylate) |
