AMG-221

• UNSPSC Description:

  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].

• Target Antigen:

  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 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.

• Shipping Conditions:

  Room temperature

• Clinical Information:

  Phase 1

• CAS Number:

  1095565-81-3