BMS-665053 | CAS#1173435-64-7 | MedKoo Biosciences

MedKoo Cat#: 530525 | Name: BMS-665053

Description:

WARNING: This product is for research use only, not for human or veterinary use.

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.

Chemical Structure

BMS-665053

CAS#1173435-64-7

Theoretical Analysis

MedKoo Cat#: 530525

Name: BMS-665053

CAS#: 1173435-64-7

Chemical Formula: C16H14Cl3F2N3O2

Exact Mass: 423.0120

Molecular Weight: 424.65

Elemental Analysis: C, 45.25; H, 3.32; Cl, 25.04; F, 8.95; N, 9.90; O, 7.54

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.

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Related CAS #

No Data

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

Instruction

View handling instruction

Preparing Stock Solutions

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

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.