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产品描述 |
SKI2852 is a Highly Potent, Selective, and Orally Bioavailable Inhibitor of 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1) potentially for treatment of diabetics. SKI2852 bioactivity data: hHSD1 IC50 = 2.9nM; mHSD1 IC50 = 1.6nM; HEK293 IC50 = 4/4 nM; Mous PK: F = 96%; CYP3A4 IC50 > 10 µM; CYP2C19 IC50 > 10 µM. SKI2852 demonstrated no CYP and PXR liabilities, excellent PK profiles across species, and highly potent and sustainable PD activity. Repeated oral administration of SKI2852 significantly reduced blood glucose and HbA1c levels and improved the lipid profiles in ob/ob mice. |
化学结构 |
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化学名称 |
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 |
SMILES Code |
O=C(C1=NC(N2CCN(C[C@H]2C)C3=CC=C(C=C3F)S(C)(=O)=O)=NC=C1)N[C@@H]4[C@@H]5C[C@H]6C[C@](C5)(O)C[C@@H]4C6 |
基本信息 |
产品编号:XM347 产品名称:SKI2852 别名:SKI2852; SKI-2852; SK I2852. CAS#:1346554-47-9 分子式:C27H34FN5O4S 精确分子量:543.2316 分子量:543.6584
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物化性质 |
外观: 白色或类白色固体粉末
纯度: >98%
运输信息: 非危险化学品,适于常温或冰袋运输。
储存条件: 低温,干燥,避光。
溶解性: 溶于DMSO, 不溶于水
储存期限:3年 -20℃固体储存
2 年 -80℃ 溶液储存 |
该产品只供科研使用,不能给病人提供。
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