A GRK inhibitor (IC50s = 3.9

CCG-215022 – 5 mg

Brand:
Cayman
CAS:
1813527-81-9
Storage:
-20
UN-No:
Non-Hazardous - /

CCG-215022 is a G protein-coupled receptor kinase (GRK) inhibitor (IC50s = 3.9, 0.15, and 0.38 μM for GRK1, GRK2, and GRK5, respectively).{58101} It is selective for GRKs over protein kinase A (PKA; IC50 = 120 μM). CCG-215022 (500 nM) increases contractility in isoproterenol-stimulated isolated mouse cardiomyocytes. It prevents the desensitization of histamine H1 receptor- and purinergic P2Y2 receptor-driven phospholipase C signaling in human ULTR myometrial cells and isolated rat mesenteric smooth muscle cells (MSMCs), respectively (IC50s = 3.09 and 2.95 μM, respectively).{58102}  

 

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SKU: 31120 - 5 mg Category:

Description

A GRK inhibitor (IC50s = 3.9, 0.15, and 0.38 μM for GRK1, GRK2, and GRK5, respectively); selective for GRKs over PKA (IC50 = 120 μM); increases contractility in isoproterenol-stimulated isolated mouse cardiomyocytes at 500 nM; prevents the desensitization of histamine H1 receptor- and purinergic P2Y2 receptor-driven phospholipase C signaling in human ULTR myometrial cells and isolated rat MSMCs, respectively (IC50s = 3.09 and 2.95 μM, respectively)

Formal name: 4-[4-fluoro-3-[[(2-pyridinylmethyl)amino]carbonyl]phenyl]-1,2,3,4-tetrahydro-N-1H-indazol-5-yl-6-methyl-2-oxo-5-pyrimidinecarboxamide

Synonyms: 

Molecular weight: 499.5

CAS: 1813527-81-9

Purity: ≥98%

Formulation: A crystalline solid

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