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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-11β-HSD-SKI2852
SKI2852

Chemical Structure : SKI2852

CAS No.: 1346554-47-9

SKI2852 (SKI-2852, J2H-1702)

货号: PC-61137Not For Human Use, Lab Use Only.

SKI-2852 (J2H-1702) is a highly potent, selective, and orally bioavailable 11β-HSD1 inhibitor with IC50 of 2.9 and 1.6 nM for hHSD1 and mHSD1, respectively.

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5 mg ¥1280 In stock
10 mg ¥1980 In stock
25 mg ¥3580 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

SKI-2852 (J2H-1702) is a highly potent, selective, and orally bioavailable 11β-HSD1 inhibitor with IC50 of 2.9 and 1.6 nM for hHSD1 and mHSD1, respectively.
SKI-2852 demonstrates no CYP and PXR liabilities, excellent PK profiles across species, and highly potent and sustainable PD activity.
SKI-2852 significantly reduces blood glucose and HbA1c levels and improves the lipid profiles in ob/ob mice, synergistically enhances the HbA1c-lowering effect of metformin in vivo.

物理化学性质&存储条件

分子量 543.658
分子式 C27H34FN5O4S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

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

参考文献

1. Ryu JH, et al. J Med Chem. 2016 Nov 23;59(22):10176-10189.

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