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AMG-221

CAT: 0804-HY-10555-01Size: 10 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-10555-01Size:10 mg
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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].
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.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
Phase 1

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