| Bioactivity | BVT-14225 is a selective 11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor with an IC50 of 52 nM. | ||||||||||||
| Target | IC50: 52 nM (11β-HSD1) | ||||||||||||
| Invitro | Selective inhibition of 11β-HSD1 decreases blood glucose concentrations in hyperglycaemic mice. Selective inhibitors of 11β-HSD1 have considerable potential as treatments for a number of diseases of great unmet medical need such as type 2 diabetes, obesity and metabolic syndrome, a multifactorial disorder. BVT-14225 shows high activity in the enzyme assay with 90% inhibition at 10 μM. It has an IC50 for 11β-HSD1 on a human enzyme assay of 52 nM[2]. | ||||||||||||
| Name | BVT-14225 | ||||||||||||
| CAS | 376638-65-2 | ||||||||||||
| Formula | C16H20ClN3O3S2 | ||||||||||||
| Molar Mass | 401.93 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Barf T, et al. Arylsulfonamidothiazoles as a new class of potential antidiabetic drugs. Discovery of potent and selective inhibitors of the 11beta-hydroxysteroid dehydrogenase type 1. J Med Chem. 2002 Aug 29;45(18):3813-5. [2]. Vicker N, et al. Novel non-steroidal inhibitors of human 11beta-hydroxysteroid dehydrogenase type 1. J Steroid Biochem Mol Biol. 2007 May;104(3-5):123-9. |