CMPD101

Pricing Availability Delivery Time Qty
Cat.No. 5642 - CMPD101 | C24H21F3N6O | CAS No. 865608-11-3
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)
Datasheet
Citations
Literature

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
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.

All Tocris products are intended for laboratory research use only.

Solubility Data

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

Preparing Stock Solutions

The following data is based on the product molecular weight 466.46. Batch specific molecular weights may vary from batch to batch due to solvent 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

Safety Datasheet

References

References are publications that support the products' biological activity.

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


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Keywords: potent selective GRK2 GRK3 inhibitors inhibits receptors GPCRs desensitization kinases G Protein (Heterotrimeric)

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