WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H530525
CAS#: 1173435-64-7
Description: BMS-665053 is a corticotropin-releasing factor-1 (CRF1) receptor antagonist. BMS-665053)11 had high affinity for the CRF1 receptor (IC50 = 1.0 nM) and was a potent inhibitor of CRF-stimulated cyclic adenosine monophosphate (cAMP) production in human Y-79 retinoblastoma cells (IC50 = 4.9 nM), indicating that it behaved as an antagonist. In addition, BMS-665053 was efficacious in the Defensive Withdrawal model of anxiety in rats and had low in vivo clearance (Cl = 17 mL/min/kg, t½ = 7.8 h) in rats.
Hodoodo Cat#: H530525
Name: BMS-665053
CAS#: 1173435-64-7
Chemical Formula: C16H14Cl3F2N3O2
Exact Mass: 423.01
Molecular Weight: 424.654
Elemental Analysis: C, 45.25; H, 3.32; Cl, 25.04; F, 8.95; N, 9.90; O, 7.54
This product is not in stock, which may be available by custom synthesis.
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Synonym: BMS-665053; BMS 665053; BMS665053.
IUPAC/Chemical Name: (S)-5-chloro-1-(1-cyclopropylethyl)-3-((2,6-dichloro-4-(difluoromethoxy)phenyl)amino)pyrazin-2(1H)-one
InChi Key: NFRNVFLIULAQST-ZETCQYMHSA-N
InChi Code: InChI=1S/C16H14Cl3F2N3O2/c1-7(8-2-3-8)24-6-12(19)22-14(15(24)25)23-13-10(17)4-9(5-11(13)18)26-16(20)21/h4-8,16H,2-3H2,1H3,(H,22,23)/t7-/m0/s1
SMILES Code: ClC1=CC(OC(F)F)=CC(Cl)=C1NC2=NC(Cl)=CN([C@@H](C)C3CC3)C2=O
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
| Biological target: | |
| In vitro activity: | |
| In vivo activity: |
The following data is based on the product molecular weight 424.65 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.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | |
| In vitro protocol: | |
| In vivo protocol: |
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.
