AMG-221

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].

Product Specifications

CAS Number

[1095565-81-3]

UNSPSC

12352005

Target

11β-HSD

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease

Applications

Metabolism-sugar/lipid metabolism

Field of Research

Metabolic Disease

Assay Protocol

https://www.medchemexpress.com/amg-221.html

Solubility

10 mM in DMSO

Smiles

O=C1N=C(N[C@@H]2[C@@](C3)([H])CC[C@@]3([H])C2)S[C@@]1(C)C(C)C

Molecular Formula

C14H22N2OS

Molecular Weight

266.40

References & Citations

[1]Seb Caille, et al. Two asymmetric syntheses of AMG 221, an inhibitor of 11beta-hydroxysteroid dehydrogenase type 1.J Org Chem. 2009 May 15;74 (10) :3833-42.|[2]Murielle M Véniant, et al. Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S) -2- ((1S,2S,4R) -bicyclo[2.2.1]heptan-2-ylamino) -5-isopropyl-5-methylthiazol-4 (5H) -one (AMG 221) . J Med Chem. 2010 Jun 10;53 (11) :4481-7.|[3]Aiwen Li, et al. Synthesis and Evaluation of the Metabolites of AMG 221, a Clinical Candidate for the Treatment of Type 2 Diabetes. ACS Med Chem Lett. 2011 Sep 13;2 (11) :824-7.