CMPD101

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Chemical Structure| 865608-11-3 同义名 : -
CAS号 : 865608-11-3
货号 : A1165861
分子式 : C24H21F3N6O
纯度 : 98%+
分子量 : 466.46
MDL号 : MFCD30182336
存储条件：

Pure form Keep in dark place, sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 250 mg/mL(535.95 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
生物活性
描述 CMPD101 is a potent, highly selective, membrane-permeable small molecule inhibitor of GRK2/3, with IC50s of 18 nM and 5.4 nM, respectively. CMPD101 is less selective for GRK1, GRK5, ROCK-2 and PKCα, with IC50s of 3.1 μM, 2.3 μM, 1.4 μM and 8.1 μM, respectively. CMPD101 can be used in heart failure studies [1].Pre-treatment of CMPD101 at a concentration of 100 μM for 20 minutes inhibits β2AR internalisation, significantly reduces isoproterenol-induced formation of lattice protein-encapsulated vesicles and β2AR-GFP fusion proteins are retained at the plasma membrane of the HEK-B2 cell line [1].Pre-treatment with CMPD101 in the concentration range of 3-30 μM for 30 min partially inhibited Ser375 phosphorylation, and pre-treatment with 30 μM CMPD101 completely blocked Ser375 phosphorylation. It also inhibited the phosphorylation of MOPr Thr370, Thr376 and Thr379 residues. Meanwhile, pre-treatment with CMPD101 in the concentration range of 3-30 μM for 30 min did not affect the DAMGO-induced increase in ERK1/2 and Elk-1 phosphorylation, whereas at 30 μM, CMPD101 resulted in a small increase in basal ERK1/2 phosphorylation in HEK 293 cells expressing HA-MOPs[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.14mL

0.43mL

0.21mL

10.72mL

2.14mL

1.07mL

21.44mL

4.29mL

2.14mL
参考文献

[1]Okawa T, 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. 2017 Aug 24;60(16):6942-6990.

[2]Yu Q, et al. Inhibition of prostatic smooth muscle contraction by the inhibitor of G protein-coupled receptor kinase 2/3, CMPD101.Eur J Pharmacol. 2018 Jul 15;831:9-19.