Cat. No. 5642

CMPD101 C24H21F3N6O [865608-11-3]

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Chemical Name: 3-[[[4-Methyl-5-(4-pyridinyl)-4H-1,2,4-triazol-3-yl]methyl]amino]-N-[[2-(trifluoromethyl)phenyl]methyl]benzamide

Biological Activity

Potent and selective GRK2/3 inhibitor (IC50 values are 32 and 54 nM for GRK3 and GRK2, respectively). Exhibits selectivity for GRK2/3 over GRK1/5. Reduces DAMGO-induced desensitization and internalization of μ-opioid receptors.

Technical Data

Soluble to 100 mM in DMSO and to 100 mM in ethanol
>98 %
Store at -20°C

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch
Safety Data Sheet: View Safety Data Sheet

Lowe et al (2015) Role of G protein-coupled receptor kinases 2 and 3 in μ-opioid receptor desensitization and internalization. Mol.Pharmacol. 88 347. PMID: 26013542.

Thal et al (2011) Molecular mechanism of selectivity among G protein-coupled receptor kinase 2 inhibitors. Mol.Pharmacol. 80 294. PMID: 21596927.

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Keywords: CMPD101, supplier, potent, selective, GRK2, GRK3, inhibitors, inhibits, receptors, GPCRs, desensitization, kinases, Tocris Bioscience, G Protein (Heterotrimeric) Inhibitor products

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