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AMG-221 

目录号: HY-10555
产品使用指南

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

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AMG-221 Chemical Structure

AMG-221 Chemical Structure

CAS No. : 1095565-81-3

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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[1][2]. AMG-221 can be used for the research of type 2 diabetes[3].

体外研究
(In Vitro)

AMG-221 shows selectivity over 11β-HSD2, 17β-HSD1, and glucocorticoid receptor (GR) (IC50 values for all assays are >10 μM)[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(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[2].
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)[2].
AMG-221 has a good bioavailability in mouse, rat, and dog. However, the bioavailability in monkey is low[2].
AMG-221 exhibits moderate oral bioavailability (male CD1 mouse 31%) following oral administration (10 mg/kg)[3].
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)[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Diet-Induced Obesity (DIO) Mice[2]
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.
分子量

266.40

Formula

C14H22N2OS

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
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AMG-221
目录号:
HY-10555
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