| Identification | Back Directory | [Name]
BMS-248360 | [CAS]
254737-87-6 | [Synonyms]
BMS-248360
BMS-248360 >=98% (HPLC)
[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]- | [Molecular Formula]
C36H45N5O5S | [MDL Number]
MFCD09027363 | [MOL File]
254737-87-6.mol | [Molecular Weight]
659.84 |
| Hazard Information | Back Directory | [Uses]
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]. | [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. DOI:10.1021/jm020138n |
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