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Chemical Structure : Compound 101
CAS No.: 865608-11-3
Catalog No.: 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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 10 mg | $118 | In stock | |
| 50 mg | $328 | In stock | |
| 100 mg | $528 | In stock | |
| 500 mg | Get quote |
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Compound 101 (GRK2 inhibitor 101, Takeda compound 101, Cmpd101) is a novel membrane-permeable, small-molecule inhibitor of GRK2 and GRK3.
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.
| M.Wt | 466.468 | |
| Formula | C24H21F3N6O | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
3-(((4-methyl-5-(pyridin-4-yl)-4H-1,2,4-triazol-3-yl)methyl)amino)-N-(2-(trifluoromethyl)benzyl)benzamide |
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1. Lowe JD, et al. Mol Pharmacol. 2015 Aug;88(2):347-56.
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