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| 2-[2-[4-(4-NITROBENZYLOXY)PHENYL]ETHYL]ISOTHIOUREA MESYLATE Basic information |
| Product Name: | 2-[2-[4-(4-NITROBENZYLOXY)PHENYL]ETHYL]ISOTHIOUREA MESYLATE | | Synonyms: | Carbamimidothioic acid 2-[4-[(4-nitrophenyl)methoxy]phenyl]ethyl ester methanesulfonate;Carbamimidothioic acid 2-[4-[(4-nitrophenyl)methoxy]phenyl]ethyl ester monomethanesulfonate;KB-R7943;KB-R7943 MESYLATE;2-[2-[4-(4-NITROBENZYLOXY)PHENYL]ETHYL]ISOTHIOUREA MESYLATE;2-(2-(4-(4-NITROBENZYLOXY)PHENYL)ETHYL)ISOTHIOUREA, METHANE SULFONATE;S-[4-[(4-Nitrobenzyl)oxy]phenethyl]isothiourea Methanesulfonate;4-((4-Nitrobenzyl)oxy)phenethyl carbaMiMidothioate Methanesulfonate | | CAS: | 182004-65-5 | | MF: | C17H21N3O6S2 | | MW: | 427.5 | | EINECS: | | Product Categories: | Signalling;Ion transporter and other ion channel | | Mol File: | 182004-65-5.mol |
| 2-[2-[4-(4-NITROBENZYLOXY)PHENYL]ETHYL]ISOTHIOUREA MESYLATE Chemical Properties |
| Melting point | >214°C (dec.) | | storage temp. | Inert atmosphere,2-8°C | | solubility | Soluble in DMSO (up to 50 mg/ml). | | form | White crystalline solid | | color | Tan | | 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. |
| 2-[2-[4-(4-NITROBENZYLOXY)PHENYL]ETHYL]ISOTHIOUREA MESYLATE Usage And Synthesis |
| Description | KB-R7943 (182004-65-5) is a potent and selective inhibitor of the reversed Na+/Ca2+ exchanger (NCE or NCX; IC50‘s = 1.2-2.4 μM in cardiomyocytes, smooth muscle cells, NCX1-transfected fibroblasts1; 0.7 μM in cultured rat forebrain2). KB-R7943 has also been shown to inhibit the mitochondrial Ca2+ uniporter (MCU) Ki = 5.5 μM.3 Recently shown to inhibit complex I in the mitochondrial respiratory chain (IC50 = 11.4 μM) and block NMDA receptors (IC50 = 13.4 μM).4 | | Uses | KB-R7943 Mesylate is a selective inhibitor of the reverse mode of Na+/Ca2+ exchange in cells expressing NCX1. | | General Description | A cell-permeable inhibitor of the influx/reverse mode of the Na+/Ca2+ exchanger (NCX) (IC50 = 4.3 μM for NCX1, 4.7 μM for NCX2, and 1.4 μM for NCX3). Directly modulates Na+/Mg2+ exchange in a Ca2+-dependent manner. Reported ot offer neuronal and cardio-protection against ischemic injury. Also inhibits nicotinic acetylcholine receptors and NMDA receptor channels (IC50<10 μM). | | Biological Activity | Potent, selective inhibitor of the reverse mode of the Na + /Ca 2+ exchanger (IC 50 = 0.7 mM). Does not affect Na + -dependent transport systems, Na + channels or ionotropic glutamate receptors. | | Biochem/physiol Actions | Target IC50: 4.3 μM, 4.7 μM, and 1.4 μM for NCX1,NCX2, and NCX3, respectively | | References | 1) Iwamoto et al. (1996), Novel Isothiourea Derivative Selectively Inhibits the Reverse Mode of Na+/Ca2+ Exchange in Cells Expressing NCX1; J. Biol .Chem., 271 22391
2) Hoyt et al. (1998) Reverse Na+/Ca2+ exchange contributes to glutamate-induced intracellular Ca2+ concentration increases in cultured rat forebrain neurons; Mol. Pharmacol., 53 742
3) Santo-Domingo et al. (2007) The plasma membrane Na+/Ca2+ exchange inhibitor KB-R7943 is also a potent inhibitor of the mitochondrial Ca2+ uniporter; Br. J. Pharmacol., 151 647
4) Brustovetsky et al. (2011) KB-R7943, an inhibitor of the reverse Na+/Ca2+ exchanger, blocks N-methyl-D-aspartate receptor and inhibits mitochondrial complex I; Br. J. Pharmacol,. 162 255 |
| 2-[2-[4-(4-NITROBENZYLOXY)PHENYL]ETHYL]ISOTHIOUREA MESYLATE Preparation Products And Raw materials |
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![2-[2-[4-(4-NITROBENZYLOXY)PHENYL]ETHYL]ISOTHIOUREA MESYLATE](/img/182004-65-5.jpg "2-[2-[4-(4-NITROBENZYLOXY)PHENYL]ETHYL]ISOTHIOUREA MESYLATE")
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