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2254333-97-4

2254333-97-4 Structure

2254333-97-4 Structure
IdentificationBack Directory
[Name]

BMS-986308
[CAS]

2254333-97-4
[Synonyms]

BMS-986308
3-Pyridinecarbonitrile, 6-[4-[[(3R,5S)-3-(1,3-dihydro-4-methyl-1-oxo-5-isobenzofuranyl)-5-methyl-1-piperazinyl]methyl]-2H-1,2,3-triazol-2-yl]-4-methyl-
[Molecular Formula]

C24H25N7O2
[MOL File]

2254333-97-4.mol
[Molecular Weight]

443.5
Chemical PropertiesBack Directory
[Boiling point ]

736.3±70.0 °C(predicted)
[density ]

1.41±0.1 g/cm3(Temp: 20 °C; Press: 760 Torr)(predicted)
[pka]

8.02±0.60(predicted)
Hazard InformationBack Directory
[Uses]

BMS-986308 is a selective and orally active renal outer medullary potassium (ROMK) channel inhibitor. BMS-986308 is selective for ROMK over hERG. BMS-986308 can be used for heart failure research[1].
[in vivo]

BMS-986308 (0.01-3 mg/kg; p.o; once) demonstrates efficacy in the volume-loaded rat diuresis model[1].

Animal Model:Male Sprague-Dawley rats (age: 8-12 weeks, 270-300 g)[1]
Dosage:0.01 mg/kg, 0.03 mg/kg, 0.1 mg/kg, 0.3 mg/kg, 1 mg/kg and 3 mg/kg
Administration:p.o; once (10% v/v DMAC, 40% v/v PEG400, 50% v/v of 30% w/v of HPβCD in 50 mM citrate buffer (pH 4.0))
Result:Led to a robust increase in diuresis.
[References]

[1] Jeremy M Richter, et al. Discovery of BMS-986308: A Renal Outer Medullary Potassium Channel Inhibitor for the Treatment of Heart Failure. J Med Chem. 2024 Jun 13;67(11):9731-9744. DOI:10.1021/acs.jmedchem.4c00893
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