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BVT-14225

Names

[ CAS No. ]:
376638-65-2

[ Name ]:
BVT-14225

[Synonym ]:
4-Thiazoleacetamide, 2-[[(3-chloro-2-methylphenyl)sulfonyl]amino]-N,N-diethyl-
MFCD25976913
2-(2-{[(3-Chloro-2-methylphenyl)sulfonyl]amino}-1,3-thiazol-4-yl)-N,N-diethylacetamide

Biological Activity

[Description]:

BVT-14225 is a selective 11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor with an IC50 of 52 nM.

[Related Catalog]:

Signaling Pathways >> Others >> Others
Research Areas >> Metabolic Disease

[Target]

IC50: 52 nM (11β-HSD1)[1]


[In Vitro]

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].

[References]

[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.


[Related Small Molecules]

Captisol | Cyclosporin A | H2DCFDA | 0MPTP hydrochloride | GW4869 | Etomoxir | TD139 | Mitoquinone mesylate | GSK2795039 | JC-1 | BAPTA-AM | AP 20187 | Setanaxib (GKT137831) | D-Luciferin | Crotaline

Chemical & Physical Properties

[ Molecular Formula ]:
C16H20ClN3O3S2

[ Molecular Weight ]:
401.93

[ Appearance of Characters ]:
light yellow solid

[ Storage condition ]:
-20℃

Related Compounds