Chemical Structure : AMG221
Catalog No.: PC-20841Not For Human Use, Lab Use Only.
AMG221 is a potent, selective orally active 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1) inhibitor with Ki of 12.8 nM and cell IC50 of 10.1 nM.
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AMG221 is a potent, selective orally active 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1) inhibitor with Ki of 12.8 nM and cell IC50 of 10.1 nM.
AMG221 showed selectivity over 11β-HSD2, 17β-HSD1, and glucocorticoid receptor (GR), as well as 61 other human targets (IC50>10 uM).
AMG221 (25 and 50 mg/kg, b.i.d) significantly decreases insulin levels, reduces blood glucose in DIO mice.
M.Wt | 266.40 | |
Formula | C14H22N2OS | |
Appearance | Solid | |
Storage |
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Solubility |
10 mM in DMSO |
1. Véniant MM, et al. J Med Chem. 2010 Jun 10;53(11):4481-7.
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