CMPD101
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
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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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 -
Molecular mechanism of selectivity among G protein-coupled receptor kinase 2 inhibitors.
Thal et al.
Mol.Pharmacol., 2011;80:294 -
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.
Okawa et al.
J.Med.Chem., 2017;60:6942
Product Datasheets
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Citation for CMPD101
The citations listed below are publications that use Tocris products. Selected citations for CMPD101 include:
1 Citation: Showing 1 - 1
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Conformational signatures in β-arrestin2 reveal natural biased agonism at a G-protein-coupled receptor.
Authors: Reyes-Alcaraz Et al.
Commun Biol 2018;1:128
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