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.
Product information
CAS Number: 254737-87-6
Molecular Weight: 659.84
Formula: C36H45N5O5S
Chemical Name: 4'-({2-butyl-4-oxo-1,3-diazaspiro[4.4]non-1-en-3-yl}methyl)-N-(3,4-dimethyl-1,2-oxazol-5-yl)-2'-[(3,3-dimethyl-2-oxopyrrolidin-1-yl)methyl]-[1,1'-biphenyl]-2-sulfonamide
Smiles: CC1(C)CCN(CC2=CC(CN3C(CCCC)=NC4(CCCC4)C3=O)=CC=C2C2=CC=CC=C2S(=O)(=O)NC2ON=C(C)C=2C)C1=O
InChiKey: NBDFXMDYBLSGLX-UHFFFAOYSA-N
InChi: InChI=1S/C36H45N5O5S/c1-6-7-14-31-37-36(17-10-11-18-36)34(43)41(31)22-26-15-16-28(27(21-26)23-40-20-19-35(4,5)33(40)42)29-12-8-9-13-30(29)47(44,45)39-32-24(2)25(3)38-46-32/h8-9,12-13,15-16,21,39H,6-7,10-11,14,17-20,22-23H2,1-5H3
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
BMS-248360 shows activity against rat AT1 and rat ETA receptor, with Kis of 6.0 nM and 1.9 nM, respectively. BMS-248360 shows no activity against AT2 and ETB receptor subtypes.
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). BMS-248360 (30 µmol/kg, 100 µmol/kg; p.o.) blocks the hypertensive effects of intravenously administered AII.
Products are for research use only. Not for human use.
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