AMG221 | 11beta-HSD1 inhibitor | Probechem Biochemicals

Chemical Structure : AMG221

AMG221 (AMG 221)

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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Biological Activity

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.

Physicochemical Properties

M.Wt	266.40
Formula	C14H22N2OS
Appearance	Solid
CAS No.
Storage	Solide Powder -20°C 12 Months; 4°C 6 Months	In Solvent -80°C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	O=C1N=C(N[C@@H]2[C@@](C3)([H])CC[C@@]3([H])C2)S[C@]1(C(C)C)C

References

1. Véniant MM, et al. J Med Chem. 2010 Jun 10;53(11):4481-7.

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AMG221 (AMG 221)

Biological Activity

Physicochemical Properties

References

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