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编 号：F549505
分子式：C18H19Cl2N3O
分子量：364.27
分子式：C18H19Cl2N3O
分子量：364.27
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CAS No: 1140898-87-8
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生物活性：
BMS-823778 hydrochloride is a potent, selective and orally active 11β-HSD1 inhibitor with an IC50 of 2.3 nM against human 11β-HSD1.
体内研究：
BMS-823778 (10-100 mg/kg; oral; once) hydrochloride 在饮食诱导肥胖 (DIO) 小鼠中表现出强烈的急性药效学作用 (ED50=34 mg/kg)。Animal Model:Diet-induced obese (DIO) mice
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
Dosage:5 or 10 mg/kg
Administration:IV or PO (Pharmacokinetic Analysis)
Result:Single-Dose Pharmacokinetic Parameters of BMS-823778SpeciesRoute Dose (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
BMS-823778 hydrochloride is a potent, selective and orally active 11β-HSD1 inhibitor with an IC50 of 2.3 nM against human 11β-HSD1.
体内研究：
BMS-823778 (10-100 mg/kg; oral; once) hydrochloride 在饮食诱导肥胖 (DIO) 小鼠中表现出强烈的急性药效学作用 (ED50=34 mg/kg)。Animal Model:Diet-induced obese (DIO) mice
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
Dosage:5 or 10 mg/kg
Administration:IV or PO (Pharmacokinetic Analysis)
Result:Single-Dose Pharmacokinetic Parameters of BMS-823778SpeciesRoute Dose (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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