385585

17β-Hydroxysteroid Dehydrogenase Type-3 Inhibitor

The 17β-Hydroxysteroid Dehydrogenase Type-3 Inhibitor controls the biological activity of 17β-Hydroxysteroid Dehydrogenase Type-3.

• 別名: 17β-Hydroxysteroid Dehydrogenase Type-3 Inhibitor, 17β-HSD3 Inhibitor, 5-(3-Bromo-4-hydroxybenzylidene)-3-(4-methoxyphenyl)-2-thioxothiazolidin-4-one
• 実験式（ヒル表記法）: C₁₇H₁₂BrNO₃S₂
• CAS番号: 330203-01-5
• 分子量: 422.32
• MDL番号: MFCD22683848
• UNSPSCコード: 12352200
• NACRES: NA.77

特性

• 品質水準: 100
• アッセイ: ≥97% (HPLC)
• 形状: solid
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; protect from light
• 色: yellow
• 溶解性: DMSO: 50 mg/mL, pink
• 輸送温度: ambient
• 保管温度: 2-8°C
• SMILES記法: O=C(N(C(S/1)=S)C2=CC=C(C=C2)OC)C1=C\C3=CC=C(O)C(Br)=C3

詳細

詳細

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.

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

再構成

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

その他情報

Harada, K., et al. 2012. Bioorg. Med. Chem. Lett.22, 504.

法的情報

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 2
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable