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GRK2-IN-115h hydrochloride

Chemical Structure : GRK2-IN-115h hydrochloride

CAS No.: 1941168-71-3

GRK2-IN-115h hydrochloride (GRK2 inhibitor 115h hydrochloride)

Catalog No.: PC-60353Not For Human Use, Lab Use Only.

A highly potent and selective GRK2 inhibitor with IC50 of 18 nM.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

A highly potent and selective GRK2 inhibitor with IC50 of 18 nM; showes enough selectivity against GRK1/5/6/7, ROCK2 and PKCα with equipotent inhibition to GRK3 (IC50=5.4 nM); potentiates βAR-mediated cAMP accumulation and prevents internalization of βARs in β2AR-expressing HEK293 cells treated with isoproterenol; a novel potential agent for heart failure treatment.

Physicochemical Properties

M.Wt 502.926
Formula C24H22ClF3N6O
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

3-(((4-methyl-5-(pyridin-4-yl)-4H-1,2,4-triazol-3-yl)methyl)amino)-N-(2-(trifluoromethyl)benzyl)benzamide hydrochloride

References

1. Okawa T, et al. J Med Chem. 2017 Aug 24;60(16):6942-6990.

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