1. Membrane Transporter/Ion Channel
  2. Na+/Ca2+ Exchanger

KB-R7943 mesylate 

Cat. No.: HY-15415 Purity: 99.39%
Handling Instructions

KB-R7943 mesylate is a widely used inhibitor of the reverse Na+/Ca2+ exchanger (NCXrev) with IC50 of 5.7±2.1 µM.

For research use only. We do not sell to patients.

KB-R7943 mesylate Chemical Structure

KB-R7943 mesylate Chemical Structure

CAS No. : 182004-65-5

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10 mM * 1 mL in DMSO USD 112 In-stock
Estimated Time of Arrival: December 31
10 mg USD 102 In-stock
Estimated Time of Arrival: December 31
50 mg USD 360 In-stock
Estimated Time of Arrival: December 31
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Description

KB-R7943 mesylate is a widely used inhibitor of the reverse Na+/Ca2+ exchanger (NCXrev) with IC50 of 5.7±2.1 µM.

IC50 & Target

IC50: 5.7±2.1 µM (Na+/Ca2+ exchanger)[1]

In Vitro

KB-R7943 mesylate blocks NMDAR-mediated ion currents, and inhibits NMDA-induced increase in cytosolic Ca2+ with IC50=13.4±3.6 µM but accelerates calcium deregulation and mitochondrial depolarization in glutamate-treated neurons. KB-R7943 depolarizes mitochondria in a Ca2+-independent manner. KB-R7943 inhibits 2,4-dinitrophenol-stimulated respiration of cultured neurons with IC50=11.4±2.4 µM. In addition to NCXrev, KB-R7943 dose-dependently and reversibly blocked ion currents elicited by NMDA. KB-R7943 dose-dependently inhibits NMDA-induced increases in [Ca2+]c with IC50=13.4±3.6 µM confirming the inhibition of NMDA receptors observed in electrophysiological experiments[1]. wtRyR1-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 Ca2+ release elicited by 1 mM compared with 0.5 and 0.75 mM (60 versus 58 versus 37%, p<0.05, respectively)[2]. KB-R7943 inhibits both IhERG and native IKr rapidly on membrane depolarization with IC50 values of ~89 and ~120 nM, respectively, for current tails at −40 mV following depolarizing voltage commands to +20 mV. IhERG inhibition by KB-R7943 exhibits both time- and voltage-dependence but shows no preference for inactivated over activated channels[3].

Solvent & Solubility
In Vitro: 

DMSO : ≥ 27 mg/mL (63.16 mM)

H2O : 4.3 mg/mL (10.06 mM; Need warming)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3392 mL 11.6959 mL 23.3918 mL
5 mM 0.4678 mL 2.3392 mL 4.6784 mL
10 mM 0.2339 mL 1.1696 mL 2.3392 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[2]

EK 293 cells stably expressing the wtRyR1 (wtRyR1-HEK 293) are maintained in Dulbecco's modified Eagle's medium supplemented with 2 mM glutamine, 100 μg/mL streptomycin, 100 U/mL penicillin, 1 mM sodium pyruvate, and 10% fetal bovine serum at 37°C under 5% CO2. wtRyR1-HEK 293 cells are loaded with 5 μM Fluo-4 acetoxymethyl ester at 37°C for 30 min to measure Ca2+ transients in an imaging buffer consisting of 140 mM NaCl, 5 mM KCl, 2 mM MgCl2, 2 mM CaCl2, 10 mM HEPES, and 10 mM glucose, pH 7.4, supplemented with 0.05% bovine serum albumin. The cells are washed three times with imaging buffer and additionally incubated for 20 min at room temperature. Dye-loaded cells are washed three times with imaging buffer and imaged with a charge-coupled device camera with a 40× objective lens attached to an IX-71 microscope. The sequence of images is captured and monitored using EasyRatioPro. Caffeine dissolved in the imaging buffer is focally applied for 15 s using AutoMate Scientific. KB-R7943 is dissolved in the imaging buffer, and wtRyR1-HEK 293 cells are incubated for 10 min before the application of caffeine[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

427.50

Formula

C₁₇H₂₁N₃O₆S₂

CAS No.

182004-65-5

SMILES

NC(SCCC1=CC=C(OCC2=CC=C([N+]([O-])=O)C=C2)C=C1)=N.CS(=O)(O)=O

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Purity: 99.39%

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Product Name:
KB-R7943 mesylate
Cat. No.:
HY-15415
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KB-R7943 mesylate

Cat. No.: HY-15415