半岛bd体育手机客户端 说明
一般描述
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.
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.
包装
10 mg in Glass bottle
Packaged under inert gas
警告
Toxicity: Standard Handling (A)
重悬
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
其他说明
Harada, K., et al. 2012.Bioorg. Med. Chem. Lett.22,504.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
基本信息
经验(实验)分子式 | C17H12BrNO3S2 |
分子量 | 422.32 |
MDL编号 | MFCD22683848 |
半岛bd体育手机客户端 性质
质量水平 | 100 |
测定 | ≥97% (HPLC) |
形式 | solid |
manufacturer/tradename | Calbiochem? |
储存条件 | OK to freeze protect from light |
颜色 | yellow |
溶解性 | DMSO: 50 mg/mL, pink |
运输 | ambient |
储存温度 | 2-8℃ |
SMILES string | O=C(N(C(S/1)=S)C2=CC=C(C=C2)OC)C1=C\C3=CC=C(O)C(Br)=C3 |
安全信息
储存分类代码 | 11 - Combustible Solids |
WGK | WGK 2 |
闪点(F) | Not applicable |
闪点(C) | Not applicable |
Sigma-Aldrich