ChemicalBook--->CAS DataBase List--->1140898-87-8

1140898-87-8

1140898-87-8 Structure

1140898-87-8 Structure
IdentificationBack Directory
[Name]

BMS-823778 (BMS823778)
[CAS]

1140898-87-8
[Synonyms]

BMS-823778
BMS-823778 (BMS823778)
BMS-823778 >=98% (HPLC)
BMS 823778 hydrochloride
[Molecular Formula]

C18H19Cl2N3O
[MDL Number]

MFCD30718574
[MOL File]

1140898-87-8.mol
[Molecular Weight]

364.27
Hazard InformationBack Directory
[Uses]

BMS 823778 is a potent and selective inhibitor of human 11β-?hydroxysteroid dehydrogenase type 1 (11β-?HSD-?1) enzyme.
[in vivo]

BMS-823778 (10-100 mg/kg; oral; once) hydrochloride exhibits robust acute pharmacodynamic effects in diet-induced obese (DIO) mice (ED50=34 mg/kg) [1].

Animal Model:Diet-induced obese (DIO) mice[1]
Dosage:10-100 mg/kg
Administration:Oral, once
Result:Inhibition of 11β-HSD-1 was observed as a measure of decrease in the plasma concentration of corticosterone. The ED50 was 34 mg/kg.
Animal Model:Male Balb/C mice[1]
Dosage:5 or 10 mg/kg
Administration:IV or PO (Pharmacokinetic Analysis)
Result:Single-Dose Pharmacokinetic Parameters of BMS-823778[1]
SpeciesRouteDose (mg/kg)Cmax (μM)Tmax (h)AUC(0-24 h) (μM?h)T1/2 (h)CLTp (mL/min/kg)Vss (L/kg)F (%)
MouseIV*5--1065.22.31.2-
PO**1010.6 ± 1.3395---44

*PO Vehicle: 0.5% Methocel/0.1% Tween 80
** IV vehicle: 10% ethanol/30% propylene glycol/60% normal saline
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