CMPD101
Tocris Bioscience, part of Bio-Techne | Catalog # 5642
Potent and selective GRK2/3 inhibitor
Key Product Details
Description
Potent and selective GRK2/3 inhibitor
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
Molecular Weight
466.46
Formula
C24H21F3N6O
Storage
Store at -20°C
Purity
≥98% (HPLC)
Chemical Name
3-[[[4-Methyl-5-(4-pyridinyl)-4H-1,2,4-triazol-3-yl]methyl]amino]-N-[[2-(trifluoromethyl)phenyl]methyl]benzamide
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.
Solubility
| 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 all 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 |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
References are publications that support the biological activity of the 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 Specific Notices for CMPD101
For research use only
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