SKI2852

SKU: orb1699286

Description

SKI2852 is a potent, selective, and orally bioavailable inhibitor of 11β-HSD1. It has demonstrated efficacy in ameliorating metabolic syndrome parameters in diabetic rodent models, supporting its use in research on type 2 diabetes, obesity, and glucocorticoid metabolism.

Research Area

Metabolism Research

Key Properties

• CAS Number: 1346554-47-9
• MW: 543.65
• Purity: 99.89% (May vary between batches)
• Formula: C₂₇H₃₄FN₅O₄S
• SMILES: N(C(=O)C1=NC(=NC=C1)N2[C@H](C)CN(CC2)C3=C(F)C=C(S(C)(=O)=O)C=C3)[C@@H]4[C@]5(CC6(O)C[C@@]4(CC(C5)C6)[H])[H]
• Target: Dehydrogenase

Bioactivity

• Target IC50:
  HSD1 (human):2.9 nM|HSD1 (Ms):1.6 nM
• In Vivo:
  Oral treatment with SKI2852 (12.5 mg/kg) significantly reduced weight gain in severely obese ob/ob mice. Results of SKI2852 (1, 3 or 10 mg/kg once daily for 8.5 weeks, administered orally) showed that all doses of SKI2852 significantly reduced FFA levels. Inhibition of 11βHSD1 by SKI2852 (12.5 mg/kg) may improve systemic and hepatic insulin sensitivity and reverse diabetic symptoms by at least partially inhibiting these gluconeogenic enzyme expression levels in DIO mice.
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• In Vitro:
  SKI2852, an inhibitor of 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1), has IC 50 values of 2.9 nM and 1.6 nM for HEK293 cells transfected with human (h11βHSD1) and mouse 11βHSD1 (m11βHSD1), respectively.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

SKI 2852, SKI2852, SKI-2852, SK I 2852, SK I2852, SK I-2852

Compound Identifiers

PubChem CID

135905445