| Bioactivity | SKI2852 is a potent, selective and orally active 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor with IC50s of 1.6 nM and 2.9 nM against mHSD1 and hHSD1, respectively[1]. |
| Target | IC50: 1.6 nM (mHSD1), 2.9 nM (hHSD1) |
| Invitro | SKI2852 在稳定转染人 11β-HSD1 cDNA 的 HEK293 细胞中抑制 11β-HSD1 的 IC50 为 4.4 ± 0.5 nM[1]。SKI2852 的酰胺羰基与 Ser170 的羟基侧链建立了中心氢键相互作用，Ser170 是确定11β-HSD1 活性的催化三联体之一 (Ser170, Tyr183 和 Lys 187)[1]。 |
| In Vivo | SKI2852 (20 mg/kg; oral; once daily for 25 days) 可显著降低 ob/ob 小鼠的血糖和 HbA1c 水平，并改善脂质谱[1]。In Vivo PK Data for SKI2852[1]species |
| Name | SKI2852 |
| CAS | 1346554-47-9 |
| Formula | C27H34FN5O4S |
| Molar Mass | 543.65 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Ryu JH, et al. 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 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1). J Med Chem. 2016 Nov 23;59(22):10176-10189. |