SKI-2852( SKI 2852 | SKI2852 )

Catalog No. M11401 CAS No. 1346554-47-9

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Product Name

SKI-2852
Note

Research use only, not for human use.
Brief Description

A highly potent, selective, and orally bioavailable 11β-HSD1 inhibitor with IC50 of 2.9 and 1.6 nM for hHSD1 and mHSD1, respectively.
Description

A highly potent, selective, and orally bioavailable 11β-HSD1 inhibitor with IC50 of 2.9 and 1.6 nM for hHSD1 and mHSD1, respectively; demonstrates no CYP and PXR liabilities, excellent PK profiles across species, and highly potent and sustainable PD activity; 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.
In Vitro

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In Vivo

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Synonyms

SKI 2852 | SKI2852
Pathway

Metabolic Enzyme/Protease
Target

11β-HSD
Recptor

11β-HSD
Research Area

——
Indication

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CAS Number

1346554-47-9
Formula Weight

543.658
Molecular Formula

C27H34FN5O4S
Purity

>98% (HPLC)
Solubility

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SMILES

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
Chemical Name

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

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

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