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Product Details

KB-R7943 mesylate | TRPC channel blocker

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

References/Citations
1) Iwamoto et al. (1996), Novel Isothioures 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

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KB-R7943 mesylate | 182004-65-5 | Structure | Supplier

Catalog#  10-1163

$65.00
Quantity
Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee.
 
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CAS:
182004-65-5
Catalog Number:
10-1163
Activity:
TRPC channel blocker
Chemical Name:
2-[2-[4-(4-Nitrobenzyloxy)phenyl]ethyl]isothiourea mesylate
Molecular Weight:
427.49
Molecular Formula:
C16H17N3O3S CH3SO3H
Solubility:
Soluble in DMSO (up to 50 mg/ml).
Physical Properties:
Tan solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
RT
Stability:
Stable for 2 years as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

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