KB-R7943
2-[2-[4-(4-NITROBENZYLOXY)PHENYL]ETHYL]ISOTHIOUREA MESYLATE
CAS: 182004-65-5
Molecular Formula: C17H21N3O6S2
KB-R7943 - Names and Identifiers
| Name | 2-[2-[4-(4-NITROBENZYLOXY)PHENYL]ETHYL]ISOTHIOUREA MESYLATE |
| Synonyms | KB-R7943 KB-R7943 MESYLATE 2-[2-[4-(4-NITROBENZYLOXY)PHENYL]ETHYL]ISOTHIOUREA MESYLATE S-[4-[(4-Nitrobenzyl)oxy]phenethyl]isothiourea Methanesulfonate 4-((4-Nitrobenzyl)oxy)phenethyl carbaMiMidothioate Methanesulfonate 2-(2-(4-(4-NITROBENZYLOXY)PHENYL)ETHYL)ISOTHIOUREA, METHANE SULFONATE Carbamimidothioic acid 2-[4-[(4-nitrophenyl)methoxy]phenyl]ethyl ester methanesulfonate Carbamimidothioic acid 2-[4-[(4-nitrophenyl)methoxy]phenyl]ethyl ester monomethanesulfonate |
| CAS | 182004-65-5 |
| InChI | InChI=1/C16H17N3O3S.CH4O3S/c17-16(18)23-10-9-12-3-7-15(8-4-12)22-11-13-1-5-14(6-2-13)19(20)21;1-5(2,3)4/h1-8H,9-11H2,(H3,17,18);1H3,(H,2,3,4) |
KB-R7943 - Physico-chemical Properties
| Molecular Formula | C17H21N3O6S2 |
| Molar Mass | 427.5 |
| Melting Point | >214°C (dec.) |
| Boling Point | 534.6°C at 760 mmHg |
| Flash Point | 277.1°C |
| Solubility | Soluble in DMSO (up to 50 mg/ml). |
| Vapor Presure | 1.67E-11mmHg at 25°C |
| Appearance | White crystalline solid |
| Color | Tan |
| Storage Condition | Inert atmosphere,2-8°C |
| Stability | Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months. |
| In vitro study | KB-R7943 mesylate blocks NMDAR-mediated ion currents, and inhibits NMDA-induced increase in cytosolic Ca 2+ with IC 50 =13.4±3.6 µM but accelerates calcium deregulation and mitochondrial depolarization in glutamate-treated neurons. KB-R7943 depolarizes mitochondria in a Ca 2+ -independent manner. KB-R7943 inhibits 2,4-dinitrophenol-stimulated respiration of cultured neurons with IC 50 =11.4±2.4 µM. In addition to NCX rev , KB-R7943 dose-dependently and reversibly blocked ion currents elicited by NMDA. KB-R7943 dose-dependently inhibits NMDA-induced increases in [Ca 2+ ] c with IC 50 =13.4±3.6 µM confirming the inhibition of NMDA receptors observed in electrophysiological experiments. wt RyR1-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 Ca 2+ release elicited by 1 mM compared with 0.5 and 0.75 mM (60 versus 58 versus 37%, p<0.05, respectively). KB-R7943 inhibits both I hERG and native I Kr rapidly on membrane depolarization with IC 50 values of ~89 and ~120 nM, respectively, for current tails at −40 mV following depolarizing voltage commands to +20 mV. I hERG inhibition by KB-R7943 exhibits both time- and voltage-dependence but shows no preference for inactivated over activated channels. |
KB-R7943 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.339 ml | 11.696 ml | 23.392 ml |
| 5 mM | 0.468 ml | 2.339 ml | 4.678 ml |
| 10 mM | 0.234 ml | 1.17 ml | 2.339 ml |
| 5 mM | 0.047 ml | 0.234 ml | 0.468 ml |
Last Update：2024-01-02 23:10:35
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