Catalog Number: 5642
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
  • M.Wt:
    466.46
  • Formula:
    C24H21F3N6O
  • Solubility:
    Soluble to 100 mM in DMSO and to 100 mM in ethanol
  • Purity:
    >98%
  • Storage:
    Store at -20°C
  • CAS No:
    865608-11-3
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.
Background References
  1. Role of G protein-coupled receptor kinases 2 and 3 in μ-opioid receptor desensitization and internalization.
    Lowe et al.
    Mol.Pharmacol., 2015;88:347
  2. Molecular mechanism of selectivity among G protein-coupled receptor kinase 2 inhibitors.
    Thal et al.
    Mol.Pharmacol., 2011;80:294

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