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17β-Hydroxysteroid Dehydrogenase Type-3 Inhibitor-Calbiochem
产品编号: | 4152862 |
规格: | The 17β-Hydroxysteroid Dehydrogenase Type-3 Inhibitor controls the biological activity of 17β-Hydroxysteroid Dehydrogenase Type-3. |
包装规格: | 10 MG |
产品类别: | 进口试剂 |
品牌: | Sigma-Aldrich |
优惠价: | 立即咨询 |
产品别名
17β-Hydroxysteroid Dehydrogenase Type-3 Inhibitor-Calbiochem
17β-HSD3 Inhibitor, 5-(3-Bromo-4-hydroxybenzylidene)-3-(4-methoxyphenyl)-2-thioxothiazolidin-4-one
结构式
基本信息
Empirical Formula【经验(实验)分子式】 | C17H12BrNO3S2 |
Molecular weight | 422.32 |
MDL number | MFCD22683848 |
General description【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. |
Warning【警告】 | Toxicity: Standard Handling (A) |
Reconstitution【重悬】 | Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C. |
Other Notes【其他说明】 | Harada, K., et al. 2012. Bioorg. Med. Chem. Lett.22, 504. |
Legal Information【法律信息】 | CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany |
产品性质
Quality Level【质量水平】 | 100 |
Assay【测定】 | ≥97% (HPLC) |
form【形式】 | solid |
manufacturer/tradename | Calbiochem® |
storage condition【储存条件】 | OK to freeze protect from light |
color【颜色】 | yellow |
solubility【溶解性】 | DMSO: 50 mg/mL, pink |
shipped in【运输】 | ambient |
storage temp.【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 |
packaging【包装】 | 10 mg in Glass bottle Packaged under inert gas |
安全信息
Storage Class Code【储存分类代码】 | 11 - Combustible Solids |
WGK | WGK 2 |