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Chemical Structure| 182004-65-5 Chemical Structure| 182004-65-5

Structure of KB-R7943 mesylate
CAS No.: 182004-65-5

Chemical Structure| 182004-65-5

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KB-R7943 Mesylate is a potent and selective inhibitor used to reverse mode of the Na+/Ca2+ exchanger with IC50 value of 0.7 μM. It also inhibits the mitochondrial Ca2+ uniporter with IC50 value of 5.5 μM.

Synonyms: KB-R7943 (mesylate)

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Product Details of KB-R7943 mesylate

CAS No. :182004-65-5
Formula : C17H21N3O6S2
M.W : 427.50
SMILES Code : NC(SCCC1=CC=C(OCC2=CC=C([N+]([O-])=O)C=C2)C=C1)=N.CS(=O)(O)=O
Synonyms :
KB-R7943 (mesylate)
MDL No. :MFCD00952138
InChI Key :WGIKEBHIKKWJLG-UHFFFAOYSA-N
Pubchem ID :9823846

Safety of KB-R7943 mesylate

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
WT atrial myocytes 1 µM Heart Rhythm. 2018 Aug;15(8):1233-1241
human embryonic stem cells (H9 and H7) 100 µmol/L KB-R7943, as an NCX inhibitor, induced rapid Ca2+ transients in both H9 and H7 human embryonic stem cells, indicating the functional role of NCX in hESCs. Acta Pharmacol Sin. 2017 Dec;38(12):1663-1672
porcine retinal venules 10 μmol/L 30 minutes KB-R7943 inhibited the hyperglycemia-enhanced constriction of retinal venules to ET-1, U46619, and norepinephrine. Diabetes. 2019 Aug;68(8):1624-1634
Pak1−/− atrial myocytes 1 µM 15 minutes KB-R7943 attenuated the AngII-induced increase in diastolic [Ca2+]i and Ca2+ transient amplitude in Pak1−/− cells Heart Rhythm. 2018 Aug;15(8):1233-1241
human induced pluripotent stem cell-derived cardiomyocytes (iPSC-CMs) 3 µM or 10 µM 4-5 minutes KB-R7943 blocked the arrhythmias caused by -AA+YWF treatment, indicating the role of NCX reverse mode in arrhythmogenesis. Int J Mol Sci. 2024 Apr 30;25(9):4932
Paediatric glioblastoma cell line SF188 0.1–100 μM 72 hours KB-R7943 inhibited the viability of SF188 cells in a dose-dependent manner. Br J Pharmacol. 2019 Aug;176(15):2691-2707
Human glioblastoma cell line U251 0.1–100 μM 72 hours KB-R7943 inhibited the viability of U251 cells, reducing it to 50–60%, 7–18%, and 2–3% of control level at 20, 50, and 100 μM concentrations, respectively. Br J Pharmacol. 2019 Aug;176(15):2691-2707

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Rats Neonatal monosodium glutamate (MSG)-treated rat model Intracerebroventricular injection 62.5 pmol Single administration To evaluate the control effect of KB-R7943 on 4-aminopyridine (4-AP)-induced epileptiform activity. Results showed that KB-R7943 significantly reduced 4-AP-induced epileptiform activity in MSG-treated rats. J Biomed Sci. 2017 May 9;24(1):27
Rat Isolated rat heart ischemia/reperfusion injury model Perfusion 10 μM 1 min before and 3-min throughout the Ca2+-free solution perfusion, as well as 3 min after restoring normal KH solution KB-R7943 alleviated heart injury and calpain activity Cell Death Dis. 2020 May 21;11(5):388
Pigs Streptozotocin-induced diabetes model Extraluminal pretreatment 10 μmol/L Single treatment, lasting at least 30 minutes KB-R7943 inhibited the hyperglycemia-enhanced constriction of retinal venules to ET-1, U46619, and norepinephrine. Diabetes. 2019 Aug;68(8):1624-1634

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.34mL

0.47mL

0.23mL

11.70mL

2.34mL

1.17mL

23.39mL

4.68mL

2.34mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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