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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
产品价格
产品编号包装单位单价(元)国内现货国外库存询价单
415286210 MG2820
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
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