SKI2852|1346554-47-9--Shanghai xingMo Biotechnology

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Description

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.

Chemical Structure

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

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

Theoretical Analysis

XingMo Cat#:XM347
Product Name:SKI2852
Synonyms:SKI2852; SKI-2852; SK I2852.
CAS#:1346554-47-9
Chemical Formula:C₂₇H₃₄FN₅O₄S
Exact Mass:543.2316
Molecular Weight:543.6584

Technical Data

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 ℃ for short term (days to weeks) or -20 ℃ for long term (months to years)

Solubility: Soluble in DMSO, not in water

Shelf Life:

>2 years if stored properly.

Drug Formulation:

This drug may be formulated in DMSO

Stock Solution Storage:

0 - 4 ℃ for short term (days to weeks), or -20 ℃ for long term (months).

WARNING: This product is for research use only, not for human or veterinary use

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