A GRK2 and GRK3 inhibitor
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CMPD101

Item No. 26808

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-[[[4-methyl-5-(4-pyridinyl)-4H-1,2,4-triazol-3-yl]methyl]amino]-N-[[2-(trifluoromethyl)phenyl]methyl]-benzamide
CAS Number
865608-11-3
Molecular Formula
C24H21F3N6O
Formula Weight
466.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMSO: 20 mg/mlEthanol: 10 mg/ml
λmax
224, 247, 320 nm
SMILES
O=C(C1=CC=CC(NCC2=NN=C(C3=CC=NC=C3)N2C)=C1)NCC4=CC=CC=C4C(F)(F)F
InChi Code
InChI=1S/C24H21F3N6O/c1-33-21(31-32-22(33)16-9-11-28-12-10-16)15-29-19-7-4-6-17(13-19)23(34)30-14-18-5-2-3-8-20(18)24(25,26)27/h2-13,29H,14-15H2,1H3,(H,30,34)
InChi Key
WFOVEDJTASPCIR-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $37

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    5 mg

    $117

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    10 mg

    $194

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    25 mg

    $436

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    Product Description

    CMPD101 is an inhibitor of G protein-coupled receptor kinase 2 (GRK2) and GRK3 (IC50s = 18 and 5.4 nM, respectively).1 It is selective for GRK2 and GRK3 over GRK1, GRK5, GRK6, and GRK7 (IC50s = 3,100, 2,300, >30,000, and 25,000 nM, respectively), as well as Rho-associated kinase 2 (ROCK2) and PKCα (IC50s = 1,400 and 8,100 nM, respectively). CMPD101 induces cAMP accumulation in HEK293 cells expressing human β2-adrenergic receptors (EC50 = 10 µM). In isolated human prostate strips, CMPD101 (50 µM) inhibits contractions induced by electrical field stimulation, norepinephrine, phenylephrine, endothelin-1 (Item No. 24127), and U-46619 (Item No. 16450).2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Okawa, T., Aramaki, Y., Yamamoto, M., et al. Design, synthesis, and evaluation of the highly selective and potent G-protein-coupled receptor kinase 2 (GRK2) inhibitor for the potential treatment of heart failure. J. Med. Chem. 60(16), 6942-6990 (2017).

    2. Yu, Q., Gratzke, C., Wang, Y., et al. Inhibition of prostatic smooth muscle contraction by the inhibitor of G protein-coupled receptor kinase 2/3, CMPD101. Eur. J. Pharmacol. 831, 9-19 (2018).