1095565-81-3
1095565-81-3
Chemical Structure
AMG-221
- CAS 番号: 1095565-81-3
- Formula:C14H22N2OS
- Molecular Weight:266.40
IUPAC Name: (S)-2-(((1S,2S,4R)-bicyclo[2.2.1]heptan-2-yl)amino)-5-isopropyl-5-methylthiazol-4(5H)-one
InChIKey: YCNCXQNUXCHRRX-ZHPDPMBESA-N
SMILES: O=C1N=C(N[C@@H]2[C@@](C3)([H])CC[C@@]3([H])C2)S[C@@]1(C)C(C)C
Biological Activity: 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].
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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. AMG-221 can be used for the research of type 2 diabetes. | |||||||||||||||||||||
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References
- [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. [Content Brief]
- [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. [Content Brief]
- [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. [Content Brief]
Keywords
