BMS-665053
| Code | Size | Price |
|---|
| TAR-T26855-5mg | 5mg | £850.00 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Special offer! Add £1 to your order to get a TargetMol CCK-8 Kit. Read more here. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Quantity:
| TAR-T26855-50mg | 50mg | £1,661.00 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Special offer! Add £1 to your order to get a TargetMol CCK-8 Kit. Read more here. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Quantity:
| TAR-T26855-100mg | 100mg | £2,079.00 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Special offer! Add £1 to your order to get a TargetMol CCK-8 Kit. Read more here. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Quantity:
Prices exclude any Taxes / VAT
Overview
Regulatory Status: RUO
Shipping:
cool pack
Storage:
-20℃
Documents
Further Information
Bioactivity:
BMS-665053 is a corticotropin-releasing factor-1 (CRF1) receptor antagonist (IC50 = 1.0 nM). BMS-665053)11 is a potent inhibitor of CRF-stimulated cyclic adenosine monophosphate (cAMP) production in human Y-79 retinoblastoma cells (IC50 = 4.9 nM). In addition, BMS-665053 is efficacious in the Defensive Withdrawal model of anxiety in rats and has low in vivo clearance (Cl = 17 mL/min/kg, t? = 7.8 h) in rats.
CAS:
1173435-64-7
Formula:
C16H14Cl3F2N3O2
Molecular Weight:
424.65
Purity:
0.98
SMILES:
C[C@@H](C1CC1)n1cc(Cl)nc(Nc2c(Cl)cc(OC(F)F)cc2Cl)c1=O
References
1. Hartz RA, Vrudhula VM, Ahuja VT, Grace JE, Lodge NJ, Bronson JJ, Macor JE. Synthesis and evaluation of prodrugs of corticotropin-releasing factor-1 (CRF(1)) receptor antagonist BMS-665053 leading to improved oral bioavailability. Bioorg Med Chem Lett. 2017 Mar 15;27(6):1360-1363. doi: 10.1016/j.bmcl.2017.02.015. PubMed PMID: 28223020.
2. Zhuo X, Hartz RA, Bronson JJ, Wong H, Ahuja VT, Vrudhula VM, Leet JE, Huang S, Macor JE, Shu YZ. Comparative biotransformation of pyrazinone-containing corticotropin-releasing factor receptor-1 antagonists: minimizing the reactive metabolite formation. Drug Metab Dispos. 2010 Jan;38(1):5-15. doi: 10.1124/dmd.109.028910. PubMed PMID: 19833844.