1. GPCR/G Protein
  2. Angiotensin Receptor
    Endothelin Receptor
  3. BMS-248360

BMS-248360 

Cat. No.: HY-114953
Handling Instructions

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.

For research use only. We do not sell to patients.

BMS-248360 Chemical Structure

BMS-248360 Chemical Structure

CAS No. : 254737-87-6

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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].

IC50 & 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
Molecular Weight

659.84

Formula

C₃₆H₄₅N₅O₅S

CAS No.

254737-87-6

SMILES

O=S(C1=CC=CC=C1C2=CC=C(CN3C(CCCC)=NC4(CCCC4)C3=O)C=C2CN5C(C(C)(C)CC5)=O)(NC6=C(C)C(C)=NO6)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

BMS-248360BMS248360BMS 248360Angiotensin ReceptorEndothelin ReceptorangiotensinAT1endothelinETAInhibitorinhibitorinhibit

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