CMPD101

Name: CMPD101
Brand: Tocris Bioscience
SKU: 5642

Tocris Bioscience a Bio-Techne Brand

Catalog # 5642

Citations (1)

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Key Product Details

Description:	Potent and selective GRK2/3 inhibitor
Chemical Name:	3-[[[4-Methyl-5-(4-pyridinyl)-4H-1,2,4-triazol-3-yl]methyl]amino]-N-[[2-(trifluoromethyl)phenyl]methyl]benzamide
Purity:	≥98% (HPLC)
Molecular Weight:	466.46

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Biological Activity for CMPD101

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.

Technical Data for CMPD101

M. Wt	466.46
Formula	C₂₄H₂₁F₃N₆O
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	865608-11-3
PubChem ID	11677079
InChi Key	WFOVEDJTASPCIR-UHFFFAOYSA-N
Smiles	CN1C(CNC2=CC(C(NCC3=CC=CC=C3C(F)(F)F)=O)=CC=C2)=NN=C1C4=CC=NC=C4

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.

Solubility for CMPD101

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	46.65	100
	ethanol	46.65	100

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 will affect the solvent volumes required to prepare stock solutions.

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

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References for CMPD101

References are publications that support the biological activity of the product.

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
Thal Molecular mechanism of selectivity among G protein-coupled receptor kinase 2 inhibitors. Mol.Pharmacol. 2011 PMID: 21596927

Citations for CMPD101 (1)

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Citations are publications that use Bio-Techne products. Selected citations for CMPD101 include:

Reyes-Alcaraz et al. (2018) Conformational signatures in β-arrestin2 reveal natural biased agonism at a G-protein-coupled receptor. Commun Biol. 1:128
PMID: 30272007

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