A GRK inhibitor
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CCG-215022

Item No. 31120

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
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
CAS Number
1813527-81-9
Molecular Formula
C26H22FN7O3
Formula Weight
499.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 1 mg/mlDMSO: 1 mg/mlDMSO:PBS (pH 7.2) (1:5): 0.16 mg/ml
SMILES
O=C1NC(C)=C(C(NC2=CC(C=NN3)=C3C=C2)=O)C(C4=CC(C(NCC5=CC=CC=N5)=O)=C(F)C=C4)N1
InChi Code
InChI=1S/C26H22FN7O3/c1-14-22(25(36)32-17-6-8-21-16(10-17)12-30-34-21)23(33-26(37)31-14)15-5-7-20(27)19(11-15)24(35)29-13-18-4-2-3-9-28-18/h2-12,23H,13H2,1H3,(H,29,35)(H,30,34)(H,32,36)(H2,31,33,37)
InChi Key
BLMBNKDQXGINRE-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $49

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    5 mg

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    10 mg

    $283

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    25 mg

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    Product Description

    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).1 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).2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Homan, K.T., Waldschmidt, H.V., Glukhova, A., et al. Crystal structure of G protein-coupled receptor kinase 5 in complex with a rationally designed inhibitor. The Journal of Biological Chemisty 290(34), 20649-20659 (2015).

    2. Rainbow, R.D., Brennan, S., Jackson, R., et al. Small-molecule G protein-coupled receptor kinase inhibitors attenuate G protein-coupled receptor kinase 2-mediated desensitization of vasoconstrictor-induced arterial contractions. Mol. Pharmacol. 94(3), 1079-1091 (2018).