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AMG-221

CAS No. : 1095565-81-3

MCE 站：AMG-221

产品活性：AMG-221 是 11β-羟基类固醇脱氢酶 1 (11β-HSD1) 抑制剂， K_i 为 12.8 nM，IC₅₀ 为 10.1 nM。AMG-221 可用于 2 型糖尿病的研究。

研究领域：Others

作用靶点：Others

In Vitro: AMG-221 shows selectivity over 11β-HSD2, 17β-HSD1, and glucocorticoid receptor (GR) (IC₅₀?values for all assays are >10 μM).

In Vivo: 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).

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