CMPD101 is a novel, potent and selective G-protein coupled receptor kinase 2 and 3 (GRK2/GRK3) inhibitor (IC50 values are 35 and 32 nM at GRK2 and GRK3 respectively). CMPD101 exhibits selectivity for GRK2/3 over GRK1/5 and reduces DAMGO-induced desensitization and internalization of μ-opioid receptors. CMPD101 has been shown to potentiate phosphatidylinositol 4,5-bisphosphate (PIP2) depletion and slow agonist-induced desensitization of protease-activated receptor 2 (PAR2).
CAS Number: 865608-11-3
Molecular Weight: 466.46
Chemical Name: 3-[[[4-Methyl-5-(4-pyridinyl)-4H-1,2,4-triazol-3-yl]methyl]amino]-N-[[2-(trifluoromethyl)phenyl]methyl]benzamide
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: Soluble in DMSO, not in water
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
CMPD101 (100 μM; pre-20 mins) inhibit the internalization of β2AR, remarkably decreases the isoproterenol-induced formation of clathrin-coated vesicles and the β2AR-GFP fusion protein remained on the plasma membrane in HEK-B2 cell line. CMPD101 (3-30 μM; pre-30 minutes) produced a robust phosphorylation of Ser375, which is partially inhibited by pretreatment of cells for 30 minutes with 3 μM Cmpd101 and fully blocked by pretreatment with 30 μM Cmpd101. It also inhibits phosphorylation of MOPr at Thr370, Thr376, and Thr379 residues. CMPD101 (3-30 μM; pre-30 minutes) does not affect the DAMGO-induced increase in ERK1/2 and Elk-1 phosphorylation, at 30 μM, this compound produces a small increase in basal ERK1/2 phosphorylation in HEK 293 cells expressing HA-MOPrs.
- Lowe JD, Sanderson HS, Cooke AE, Ostovar M, Tsisanova E, Withey SL, Chavkin C, Husbands SM, Kelly E, Henderson G, Bailey CP. Role of G Protein-Coupled Receptor Kinases 2 and 3 in μ-Opioid Receptor Desensitization and Internalization. Mol Pharmacol. 2015 Aug;88(2):347-56. doi: 10.1124/mol.115.098293. Epub 2015 May 26. PubMed PMID: 26013542; PubMed Central PMCID: PMC4518089.
Products are for research use only. Not for human use.
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