KB-R7943 mesylate | NCX inhibitor

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 from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Available Options

size :PriceQuantity 
10 mg$65.00
50 mg$260.00

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 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

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 from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

Product Data Sheet:

Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. 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

20% OFF

For Postdoc
Customers!