CMPD101
Cat. No.：YN310059
CAS No. ：865608-11-3
| 产品名称: | CMPD101 |
| CAS No.: | 865608-11-3 |
| Chemical Name: | 3-[[[4-methyl-5-(4-pyridinyl)-4H-1,2,4-triazol-3-yl]methyl]amino]-N-[[2-(trifluoromethyl)phenyl]methyl]-benzamide |
| Synonyms: | GRK2 inhibitor 101;Takeda compound 101;Cmpd101 |
| 分子量: | 466.46 |
| 分子式: | C₂₄H₂₁F₃N₆O |
| SMILES: | O=C(C1=CC(NCC2=NN=C(C3=CC=NC=C3)N2C)=CC=C1)NCC4=CC=CC=C4C(F)(F)F |
| 存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
| 运输: | Room temperature in continental US; may vary elsewhere. |
| 产品描述: | CMPD101 是一种高效、高选择性、膜透性的GRK2/3小分子抑制剂，IC50分别为 18 nM 和 5.4 nM。CMPD101 针对 GRK1、GRK5 ROCK-2 和 PKCα 的选择性较小，IC50值分别为 3.1 μM，2.3 μM，1.4 μM 和 8.1 μM。CMPD101 可用于心衰疾病的研究。 |
| IC50和靶点: | [{name:"GRK2:18 nM (IC50)"},{name: "GRK3:5.4 nM (IC50)"},{name: "PKCα:8.1 μM (IC50)"},{name: "ROCK2:1.4 μM (IC50)"}] |
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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 failureJ. Med. Chem.60(16),6942-6990(2017)
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, CMPD101Eur. J. Pharmacol.831,9-19(2018)
