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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)
Citations (7)

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
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 Data for CMPD101

Solvent Max Conc. mg/mL Max Conc. mM
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.

Select a batch to recalculate based on the batch molecular weight:
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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Product Datasheets for CMPD101

Certificate of Analysis / Product Datasheet
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References for CMPD101

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

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

Okawa et al (2017) 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. 60 6942 PMID: 28699740

If you know of a relevant reference for CMPD101, please let us know.

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Keywords: CMPD101, CMPD101 supplier, potent, selective, GRK2, GRK3, inhibitors, inhibits, receptors, GPCRs, desensitization, kinases, Heterotrimeric, G-protein, GTPases, 5642, Tocris Bioscience

7 Citations for CMPD101

Citations are publications that use Tocris products. Selected citations for CMPD101 include:

Mark et al (2020) A Discrete Presynaptic Vesicle Cycle for Neuromodulator Receptors. Neuron 105 663-677.e8 PMID: 31837915

Jiri et al (2020) Mutations in GRK2 cause Jeune syndrome by impairing Hedgehog and canonical Wnt signaling. EMBO Mol Med 12 e11739 PMID: 33200460

Francesco Luigi et al (2023) Subcellular location defines GPCR signal transduction. Sci Adv 9 eadf6059 PMID: 37075112

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

Do you know of a great paper that uses CMPD101 from Tocris? Please let us know.

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