产品
编 号：F651567
分子式：C14H22N2OS
分子量：266.4
分子式：C14H22N2OS
分子量：266.4
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CAS No: 1095565-81-3
产品详情
生物活性：
AMG-221 is an inhibitor of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) with a Ki of 12.8 nM in vitro biochemical scintillation proximity assay (SPA) and an IC50 of 10.1 nM in cell-based assays. AMG-221 can be used for the research of type 2 diabetes.
体内研究：
AMG-221 (25 or 50 mg/kg;?b.i.d.; orally gavaged) inhibits 11β-HSD1 activity in DIO mice. At the end of the study, fed blood glucose shows statistically significant reduction in comparison to the vehicle group. On day 14 and after a 12 h fast, glucose tolerance is slightly improved in the AMG-221?treatment groups compared with the vehicle group. 11β-HSD1 activity is inhibited by 33%, 55%, and 47% in the inguinal fat at 4 h after?AMG-221?is orally gavaged at 5, 15, and 50 mg/kg, respectively. At 8 h, the 11β-HSD1 activity in the inguinal fat of the 5 mg/kg group has returned to a level (～10% inhibition) close to that in the control animals treated with vehicle, but there is still significant inhibition in the 15 and 50 mg/kg groups (36% and 39% inhibition, respectively). AMG-221?has a good bioavailability in mouse, rat, and dog. However, the bioavailability in monkey is low. AMG-221 exhibits moderate oral bioavailability (male CD1 mouse 31%) following oral administration (10 mg/kg).AMG-221 exhibits terminal elimination half-life (male CD1 mouse 3.32 h) due to high plasma clearance (3.31 L/h/kg) combined with large volumes of distribution (0.9 L/kg) following intravenous administration (2 mg/kg).Animal Model:Diet-Induced Obesity (DIO) Mice
Dosage:25 or 50 mg/kg (prepare in 0.1% Tween-80 and 0.5% CMC in water)
Administration:Orally gavaged; twice a day for 13 or 14 days
Result:There were statistically significant decreases in insulin levels in all treated groups when compared with the vehicle control group on day 13.
体外研究：
AMG-221 shows selectivity over 11β-HSD2, 17β-HSD1, and glucocorticoid receptor (GR) (IC50?values for all assays are >10 μM).
AMG-221 is an inhibitor of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) with a Ki of 12.8 nM in vitro biochemical scintillation proximity assay (SPA) and an IC50 of 10.1 nM in cell-based assays. AMG-221 can be used for the research of type 2 diabetes.
体内研究：
AMG-221 (25 or 50 mg/kg;?b.i.d.; orally gavaged) inhibits 11β-HSD1 activity in DIO mice. At the end of the study, fed blood glucose shows statistically significant reduction in comparison to the vehicle group. On day 14 and after a 12 h fast, glucose tolerance is slightly improved in the AMG-221?treatment groups compared with the vehicle group. 11β-HSD1 activity is inhibited by 33%, 55%, and 47% in the inguinal fat at 4 h after?AMG-221?is orally gavaged at 5, 15, and 50 mg/kg, respectively. At 8 h, the 11β-HSD1 activity in the inguinal fat of the 5 mg/kg group has returned to a level (～10% inhibition) close to that in the control animals treated with vehicle, but there is still significant inhibition in the 15 and 50 mg/kg groups (36% and 39% inhibition, respectively). AMG-221?has a good bioavailability in mouse, rat, and dog. However, the bioavailability in monkey is low. AMG-221 exhibits moderate oral bioavailability (male CD1 mouse 31%) following oral administration (10 mg/kg).AMG-221 exhibits terminal elimination half-life (male CD1 mouse 3.32 h) due to high plasma clearance (3.31 L/h/kg) combined with large volumes of distribution (0.9 L/kg) following intravenous administration (2 mg/kg).Animal Model:Diet-Induced Obesity (DIO) Mice
Dosage:25 or 50 mg/kg (prepare in 0.1% Tween-80 and 0.5% CMC in water)
Administration:Orally gavaged; twice a day for 13 or 14 days
Result:There were statistically significant decreases in insulin levels in all treated groups when compared with the vehicle control group on day 13.
体外研究：
AMG-221 shows selectivity over 11β-HSD2, 17β-HSD1, and glucocorticoid receptor (GR) (IC50?values for all assays are >10 μM).
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