SKI2852
| Code | Size | Price |
|---|
| TAR-T28796-5mg | 5mg | £850.00 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Special offer! Add £1 to your order to get a TargetMol CCK-8 Kit. Read more here. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Quantity:
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Overview
Regulatory Status: RUO
Shipping:
cool pack
Storage:
-20℃
Documents
Further Information
Bioactivity:
SKI2852 is a highly Potent, selective, and orally bioavailable inhibitor of 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1). hHSD1 IC50 = 2.9nM; mHSD1 IC50 = 1.6nM.
CAS:
1346554-47-9
Formula:
C27H34FN5O4S
Molecular Weight:
543.66
Purity:
0.98
SMILES:
C[C@@H]1CN(CCN1c1nccc(n1)C(=O)N[C@H]1[C@H]2C[C@H]3C[C@@H]1C[C@](O)(C3)C2)c1ccc(cc1F)S(C)(=O)=O
References
1. Ryu JH, Lee JA, Kim S, Shin YA, Yang J, Han HY, Son HJ, Kim YH, Sa JH, Kim JS, Lee J, Lee J, Park HG. Discovery of 2-((R)-4-(2-Fluoro-4-(methylsulfonyl)phenyl)-2-methylpiperazin-1-yl)-N-((1R,2s,3S ,5S,7S)-5-hydroxyadamantan-2-yl)pyrimidine-4-carboxamide (SKI2852): A Highly Potent, Selective, and Orally Bioavailable Inhibitor of 11?-Hydroxysteroid Dehydrogenase Type 1 (11?-HSD1). J Med Chem. 2016 Oct 31. [Epub ahead of print] PubMed PMID: 27798827.
2. Oh H, Jeong KH, Han HY, Son HJ, Kim SS, Lee HJ, Kim S, Sa JH, Jun HS, Ryu JH, Choi CS. A potent and selective 11?-hydroxysteroid dehydrogenase type 1 inhibitor, SKI2852, ameliorates metabolic syndrome in diabetic mice models. Eur J Pharmacol. 2015 Dec 5;768:139-48. doi: 10.1016/j.ejphar.2015.10.042. PubMed PMID: 26519792.