254737-87-6

254737-87-6 structure

Name: BMS-248360
Chemical Name: 2-[4-[(2-butyl-4-oxo-1,3-diazaspiro[4.4]non-1-en-3-yl)methyl]-2-[(3,3-dimethyl-2-oxopyrrolidin-1-yl)methyl]phenyl]-N-(3,4-dimethyl-1,2-oxazol-5-yl)benzenesulfonamide
CAS Number: 254737-87-6
Molecular Formula: C₃₆H₄₅N₅O₅S
Molecular Weight: 659.83800
Catalog: Signaling Pathways GPCR/G Protein Angiotensin Receptor
Create Date: 2016-11-25 02:22:23
Modify Date: 2024-01-10 22:50:58
BMS-248360 is a potent and orally active dual antagonist of both angiotensin II receptor (AT1) and endothelin A (ETA) receptor, with Kis of 10 nM and 1.9 nM for hAT1 and hETA receptor, respectively. BMS-248360 displays hypertensive effects[1].

Name	2-[4-[(2-butyl-4-oxo-1,3-diazaspiro[4.4]non-1-en-3-yl)methyl]-2-[(3,3-dimethyl-2-oxopyrrolidin-1-yl)methyl]phenyl]-N-(3,4-dimethyl-1,2-oxazol-5-yl)benzenesulfonamide
Synonyms	(1,1'-Biphenyl)-2-sulfonamide,4'-((2-butyl-4-oxo-1,3-diazaspiro(4.4)non-1-en-3-yl)methyl)-N-(3,4-dimethyl-5-isoxazolyl)-2'-((3,3-dimethyl-2-oxo-1-pyrrolidinyl)methyl) UNII-EEP77N970Y

Description	BMS-248360 is a potent and orally active dual antagonist of both angiotensin II receptor (AT1) and endothelin A (ETA) receptor, with Kis of 10 nM and 1.9 nM for hAT1 and hETA receptor, respectively. BMS-248360 displays hypertensive effects[1].
Related Catalog	Research Areas >> Cardiovascular Disease Signaling Pathways >> GPCR/G Protein >> Angiotensin Receptor Signaling Pathways >> GPCR/G Protein >> Endothelin Receptor
Target	Ki: 10 nM (hAT1), 1.9 nM (hETA receptor), 6.0 nM (rAT1), 1.9 nM(rETA receptor)[1]
In Vitro	BMS-248360 shows activity against rat AT1 and rat ETA receptor, with Kis of 6.0 nM and 1.9 nM, respectively[1]. BMS-248360 shows no activity against AT2 and ETB receptor subtypes[1].
In Vivo	BMS-248360 is found to be orally bioavailable in rats (%F=38) with excellent oral exposure (Cmax)=3.1 µM) and reasonable elimination profile (T1/2=5.5 hours)[1]. BMS-248360 (30 µmol/kg, 100 µmol/kg; p.o.) blocks the hypertensive effects of intravenously administered AII[1]. Animal Model: Male Rats[1] Dosage: 30 µM/kg, 100 µM/kg Administration: Oral administration Result: Blocked the hypertensive effects of intravenously administered AII. Animal Model: Male Rats[1] Dosage: 10 µM/kg Administration: Oral administration Result: T1/2= 5.5 hours
References	[1]. Murugesan N, et al. Discovery of N-isoxazolyl biphenylsulfonamides as potent dual angiotensin II and endothelin A receptor antagonists. J Med Chem. 2002 Aug 29;45(18):3829-35.