17beta-Hydroxysteroid Dehydrogenase Type-3 Inhibitor – Calbiochem

Descrição detalhada : A cell-permeable benzylidine-thioxothiazolidinone compound that blocks the steroidogenesis of testosterone by directly inhibiting 17β-HSD3- (17β-hydroxysteroid dehydrogenase type 3) catalyzed, NADPH-dependent, reduction of Δ4-dione C17 ketone in a Δ4-dione- (4-androstene-3,17-dione) competitive, highly potent (IC50 = 0.6, 6.0, and 40 nM, respectively, against momoset, human, and mouse 17β-HSD3 activity in testes homogenate), and selective manner, displaying no activity against 17β-HSD1 and 17β-HSD2 activity. Poor pharmacokinetic properties limit its use to culture treatments and cell-free assays only., A cell-permeable benzylidine-thioxothiazolidinone compound that blocks the steroidogenesis of the potent androgen testosterone by directly inhibiting 17β-HSD3- (17β-hydroxysteroid dehydrogenase type 3) catalyzed, NADPH-dependent, reduction of Δ4-dione C17 ketone in a Δ4-dione- (4-androstene-3,17-dione) competitive, highly potent (IC50 = 0.6, 6.0, and 40 nM, respectively, against momoset, human, and mouse 17β-HSD3 activity in testes homogenate; IC50 = 14 nM using 17β HSD3-transfected HeLa cells), and selective manner, displaying no activity against 17β-HSD1 and 17β-HSD2 activity in HeLa transfectants or AR- (andogen receptor), ERα- (estrogen receptor α), and GR- (glucocorticoid receptor) dependent transcription activities. Low aqueous solubility, lack of oral availability, and other poor pharmacokinetic properties limit its use to culture treatments and cell-free assays only.
Sinónimos : 17beta-Hydroxysteroid Dehydrogenase Type-3 Inhibitor - Calbiochem; 17beta-HSD3 Inhibitor, 5-(3-Bromo-4-hydroxybenzylidene)-3-(4-methoxyphenyl)-2-thioxothiazolidin-4-one
Fórmula molecula r: C17H12BrNO3S2
Armazenamento : 2-8C; 2-8C; 2-8C
Embalagem : 1X10MG