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SKI2852 is an orally active, selective, and efficient 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor, improving metabolic syndrome in diabetic mouse models.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $55 | In Stock | |
5 mg | $129 | In Stock | |
10 mg | $208 | In Stock |
Description | SKI2852 is an orally active, selective, and efficient 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor, improving metabolic syndrome in diabetic mouse models. |
Targets&IC50 | HSD1 (human):2.9 nM, HSD1 (Ms):1.6 nM |
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. [1] |
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. [1] |
Alias | SKI-2852 |
Molecular Weight | 543.65 |
Formula | C27H34FN5O4S |
Cas No. | 1346554-47-9 |
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] |
Relative Density. | 1.44 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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