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首页-小分子抑制剂&激动剂-Others-GRK (GPCRK)-Compound 101
Compound 101

Chemical Structure : Compound 101

CAS No.: 865608-11-3

Compound 101 (GRK2 inhibitor 101;Takeda compound 101;Cmpd101)

货号: PC-60585Not For Human Use, Lab Use Only.

Compound 101 (GRK2 inhibitor 101, Takeda compound 101, Cmpd101) is a novel membrane-permeable, small-molecule inhibitor of GRK2 and GRK3 with IC50 of 18 nM and 5.4 nM, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Compound 101 (GRK2 inhibitor 101, Takeda compound 101, Cmpd101) is a novel membrane-permeable, small-molecule inhibitor of GRK2 and GRK3 with IC50 of 18 nM and 5.4 nM, respectively.
Compound 101 inhibits the desensitization of the G protein-activated inwardly-rectifying potassium current evoked by receptor-saturating concentrations of Met-Enk, DAMGO, endomorphin-2, and morphine in rat and mouse locus coeruleus neurons.
Compound 101 produces complete inhibition of DAMGO-induced MOPr phosphorylation at Ser(375), arrestin translocation, and MOPr internalization in HEK 293 cells.

物理化学性质&存储条件

分子量 466.468
分子式 C24H21F3N6O
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

3-(((4-methyl-5-(pyridin-4-yl)-4H-1,2,4-triazol-3-yl)methyl)amino)-N-(2-(trifluoromethyl)benzyl)benzamide

参考文献

1. Lowe JD, et al. Mol Pharmacol. 2015 Aug;88(2):347-56.

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