产品
编 号：F682238
分子式：C27H34FN5O4S
分子量：543.65
分子式：C27H34FN5O4S
分子量：543.65
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CAS No: 1346554-47-9
产品详情
生物活性：
SKI2852 is a potent, selective and orally active 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor with IC50s of 1.6 nM and 2.9 nM against mHSD1 and hHSD1, respectively.
体内研究：
SKI2852 (20 mg/kg; oral; once daily for 25 days) 可显著降低 ob/ob 小鼠的血糖和 HbA1c 水平，并改善脂质谱。In Vivo PK Data for SKI2852speciesivapob
CL (L/kg/h)Vss (L/kg) t1/2 (h) AUC (μg × h/mL) Cmax (μg/mL) tmax (h) AUC (μg × h/mL) F (%)
mousec0.421.11.72.352.211.011.2696
ratc0.932.11.81.121.021.33.3960
dogd0.362.44.71.471.122.111.5298
a10% hydroxylpropyl-β-cyclodextrin was used as vehicle. b0.5% methylcellulose and 1% Tween80 was used as vehicle. cDosed iv at 1 mg/kg, po at 5mg/kg. dDosed iv at 0.5 mg/kg, po at 4 mg/kg.Animal Model:ob/ob mice, diet-induced obesity (DIO) model
Dosage:20 mg/kg
Administration:Oral, once daily for 25 days
Result:Efficiently reduced postprandial glucose and/or blood HbA1c levels and suppressed hepatic mRNA levels of gluconeogenic enzymes. Clearly enhanced hepatic and whole-body insulin sensitivities in a hyperinsulinemic-euglycemic clamp experiment in DIO mice.
Animal Model:C57BL/6 mice, rats and dogs
Dosage:0.5 or 4 mg/kg
Administration:IV or PO (Pharmacokinetic Analysis)
Result:Showed good pharmacokinetic profiles.
体外研究：
SKI2852 在稳定转染人 11β-HSD1 cDNA 的 HEK293 细胞中抑制 11β-HSD1 的 IC50 为 4.4 ± 0.5 nM。SKI2852 的酰胺羰基与 Ser170 的羟基侧链建立了中心氢键相互作用，Ser170 是确定11β-HSD1 活性的催化三联体之一 (Ser170, Tyr183 和 Lys 187)。
SKI2852 is a potent, selective and orally active 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor with IC50s of 1.6 nM and 2.9 nM against mHSD1 and hHSD1, respectively.
体内研究：
SKI2852 (20 mg/kg; oral; once daily for 25 days) 可显著降低 ob/ob 小鼠的血糖和 HbA1c 水平，并改善脂质谱。In Vivo PK Data for SKI2852speciesivapob
CL (L/kg/h)Vss (L/kg) t1/2 (h) AUC (μg × h/mL) Cmax (μg/mL) tmax (h) AUC (μg × h/mL) F (%)
mousec0.421.11.72.352.211.011.2696
ratc0.932.11.81.121.021.33.3960
dogd0.362.44.71.471.122.111.5298
a10% hydroxylpropyl-β-cyclodextrin was used as vehicle. b0.5% methylcellulose and 1% Tween80 was used as vehicle. cDosed iv at 1 mg/kg, po at 5mg/kg. dDosed iv at 0.5 mg/kg, po at 4 mg/kg.Animal Model:ob/ob mice, diet-induced obesity (DIO) model
Dosage:20 mg/kg
Administration:Oral, once daily for 25 days
Result:Efficiently reduced postprandial glucose and/or blood HbA1c levels and suppressed hepatic mRNA levels of gluconeogenic enzymes. Clearly enhanced hepatic and whole-body insulin sensitivities in a hyperinsulinemic-euglycemic clamp experiment in DIO mice.
Animal Model:C57BL/6 mice, rats and dogs
Dosage:0.5 or 4 mg/kg
Administration:IV or PO (Pharmacokinetic Analysis)
Result:Showed good pharmacokinetic profiles.
体外研究：
SKI2852 在稳定转染人 11β-HSD1 cDNA 的 HEK293 细胞中抑制 11β-HSD1 的 IC50 为 4.4 ± 0.5 nM。SKI2852 的酰胺羰基与 Ser170 的羟基侧链建立了中心氢键相互作用，Ser170 是确定11β-HSD1 活性的催化三联体之一 (Ser170, Tyr183 和 Lys 187)。
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