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KB-R7943 mesylate

Cat. No. M1927
KB-R7943 mesylate Structure
Size Price Availability Quantity
10mg USD 87 In stock
50mg USD 297 In stock
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Quality Control
Biological Activity

KB-R7943 is a plasma membrane Na(+)/Ca(2+) exchanger inhibitor. KB-R7943 reversibly inhibits inward and outward Na+/Ca2+ exchange in a dose-dependent manner (MCU; IC50 = 5.5 μM), but it does not affect Na+-dependent transport systems or ionotropic glutamate receptors. In addition, the effects of KB-R7943 on Ca(2+) homeostasis provide new evidence for the role of mitochondria modulating Ca(2+)-release and regenerative Ca(2+)-oscillations. KB-R7943 (10 and 30 microM) suppressed the tonotropic effect of ouabain, and prolonged the onset time of extra-systole induced by ouabain in isolated atria. KB-R7943 suppresses ouabain-induced arrhythmias through inhibition of the reverse-mode NCX. KB-R7943 is also a potent blocker of the transient receptor potential channels (TRPC) TRPC3, TRPC5 and TRPC6.

Protocol
Cell Experiment
Cell lines neurons, astrocytes, and microglia
Preparation method Na+-Ca2+ Exchange Activity.
Na+-Ca2+ exchange activity was determined by assaying Na+-dependent Ca2+ uptake as reported previously (Takuma et al., 1994). Briefly, the cells were preincubated in Hanks' balanced saline solution (HBSS) for 20 min, and the medium was switched to HBSS containing Ca2+ and incubated for 5 min. To increase intracellular Na+ concentration, 1 mM ouabain plus 20 μM monensin (for astrocytes and microglia) and 10 μM monensin (for neurons) were used. Monensin was added simultaneously with the isotope. Ouabain was added 5 min before monensin in astrocytes and microglia. NCX inhibitors were added 5 min before monensin and present during Ca2+ uptake reaction.
Concentrations 0~10 μ M
Incubation time 5 min
Animal Experiment
Animal models cerebral cortex (A) and striatum (B) after MCA occlusion in rats
Formulation 20% soybean oil
Dosages 3 mg/kg
Administration bolus i.v.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 427.49
Formula C16H17N3O3S.CH3SO3H
CAS Number 182004-65-5
Purity 99.48%
Solubility DMSO
Storage at -20°C
References

The plasma membrane Na+/Ca2+ exchange inhibitor KB-R7943 is also a potent inhibitor of the mitochondrial Ca2+ uniporter.
Santo-Domingo J, et al. Br J Pharmacol. 2007 Jul;151(5):647-54. PMID: 17471180.

SEA0400, a novel and selective inhibitor of the Na+-Ca2+ exchanger, attenuates reperfusion injury in the in vitro and in vivo cerebral ischemic models.
Matsuda T, et al. J Pharmacol Exp Ther. 2001 Jul;298(1):249-56. PMID: 11408549.

Effect of Na+/Ca2+ exchange inhibitor, KB-R7943 on ouabain-induced arrhythmias in guinea-pigs.
Watano T, et al. Br J Pharmacol. 1999 Aug;127(8):1846-50. PMID: 10482915.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: KB-R7943 mesylate supplier, Calcium Channel, inhibitors

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