CMPD101

Key Product Details

Product Description

CMPD101 is a 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.

Product Specifications for CMPD101

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

Preparing Stock Solutions for CMPD101

The following data is based on the product molecular weight 466.46.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.14 mL	10.72 mL	21.44 mL
5 mM	0.43 mL	2.14 mL	4.29 mL
10 mM	0.21 mL	1.07 mL	2.14 mL
50 mM	0.04 mL	0.21 mL	0.43 mL

Calculators

Background References

References are publications that support the biological activity of the product. See our Citations tab to view 38 publications citing the usage of this product.

• Thal Molecular mechanism of selectivity among G protein-coupled receptor kinase 2 inhibitors. Mol.Pharmacol. 2011 PMID: 21596927
• Okawa 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. J.Med.Chem. 2017 PMID: 28699740
• Lowe Role of G protein-coupled receptor kinases 2 and 3 in μ-opioid receptor desensitization and internalization. Mol.Pharmacol. 2015 PMID: 26013542

Product Documents for CMPD101