[CAS NO. 182004-65-5]  KB-R7943mesylate

Ships within Stock Price Qty Total
$0.00
$0.00
Please click "REQUEST A QUOTE" button if you need other sizes or custom synthesis
request a quote
If there is no stock, or you need other sizes or custom synthesis, please:

PRODUCTS SPECIFICATIONS [182004-65-5]

Catalog
HY-15415
Brand
MCE
CAS
182004-65-5

DESCRIPTION [182004-65-5]

Overview

MDLMFCD00952138
Molecular Weight427.50
Molecular FormulaC17H21N3O6S2
SMILESNC(SCCC1=CC=C(OCC2=CC=C([N+]([O-])=O)C=C2)C=C1)=N.CS(=O)(O)=O

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


Summary

KB-R7943 mesylate is a widely used inhibitor of the reverse Na + /Ca 2+ exchanger (NCX rev ) with IC 50 of 5.7±2.1 µM. KB-R7943 mesylate induces cancer cell death via activating the JNK pathway and blocking autophagic flux.


IC50 & Target

IC50: 5.7±2.1 µM (Na + /Ca 2+ exchanger) [1]


In Vitro

KB-R7943 mesylate blocks NMDAR-mediated ion currents, and inhibits NMDA-induced increase in cytosolic Ca 2+ with IC 50 =13.4±3.6 µM but accelerates calcium deregulation and mitochondrial depolarization in glutamate-treated neurons. KB-R7943 depolarizes mitochondria in a Ca 2+ -independent manner. KB-R7943 inhibits 2,4-dinitrophenol-stimulated respiration of cultured neurons with IC 50 =11.4±2.4 µM. In addition to NCX rev , KB-R7943 dose-dependently and reversibly blocked ion currents elicited by NMDA. KB-R7943 dose-dependently inhibits NMDA-induced increases in [Ca 2+ ] c with IC 50 =13.4±3.6 µM confirming the inhibition of NMDA receptors observed in electrophysiological experiments [1] . wt RyR1-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 Ca 2+ 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 I hERG and native I Kr rapidly on membrane depolarization with IC 50 values of ~89 and ~120 nM, respectively, for current tails at −40 mV following depolarizing voltage commands to +20 mV. I hERG inhibition by KB-R7943 exhibits both time- and voltage-dependence but shows no preference for inactivated over activated channels [3] .

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


Appearance

Solid


Shipping

Room temperature in continental US; may vary elsewhere.


Storage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)


Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL ( 233.92 mM ; Need ultrasonic)

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.
In Vivo:
  • 1.

    Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

    Solubility: ≥ 2.5 mg/mL (5.85 mM); Clear solution

  • 2.

    Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.85 mM); Clear solution

  • 3.

    Add each solvent one by one: 10% DMSO >> 90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.85 mM); Clear solution

* All of the co-solvents are available by MCE.


Synonyms

Carbamimidothioic acid, 2-[4-[(4-nitrophenyl)methoxy]phenyl]ethyl ester, methanesulfonate (1:1)
Carbamimidothioic acid, 2-[4-[(4-nitrophenyl)methoxy]phenyl]ethyl ester, monomethanesulfonate
2-[4-[(4-Nitrophenyl)methoxy]phenyl]ethyl carbamimidothioate methanesulfonate (1:1)
KB-R 7943