666125

Urea Transporter B Inhibitor, UTB_inh-14

• 別名: Urea Transporter B Inhibitor, UTB_inh-14, 3-(4-Ethylphenylsulfonyl)-N-(thiophen-2-ylmethyl)thieno[2,3-e][1,2,3]triazolo[1,5-a]pyrimidin-5-amine, UT-B Inhibitor, UTB Inhibitor, UTBinh14, 3-((4-Ethylphenyl)sulfonyl)-N-(2-thienylmethyl)thieno[2,3-e][1,2,3]triazolo[1,5-a]pyrimidin-5-amine
• 実験式（ヒル表記法）: C₂₀H₁₇N₅O₂S₃
• 分子量: 455.58
• UNSPSCコード: 12352200
• NACRES: NA.28

特性

• アッセイ: ≥98% (HPLC)
• 品質水準: 100
• 形状: powder
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; protect from light
• 色: white
• 溶解性: DMSO: 100 mg/mL
• 輸送温度: ambient
• 保管温度: 2-8°C

詳細

詳細

A cell-permeable triazolothienopyrimidine compound that acts as a reversible urea transporter B (UT-B)-selective inhibitor (IC50 = 10.3 and 25.1 nM against urea influx using human and mouse erythrocytes, respectively) by targeting a UT-B intracellular site in a urea-competitive manner, exhibiting little effect toward UT-A1, UT-A3, AQP1, CFTR, or TMEM16A channel activities and no cytotoxicity in MDCK cultures (100% viability after 24 h 10 µM inhibitor treatment). Shown to effectively decrease maximum urinary concentration (2.3- and 3.7-fold of basal [urea], respectively, with or without inhibitor; 300 µg/300 µl/mouse i.p.) and increase urination volume (236 vs.109 µl/4h, respectively, with or without inhibitor) from antidiuretic dDAVP- (1 µg/kg; administered 1 h after inhibitor) treated wild-type, but not UT-B^-/-, mice in vivo. Despite its short half-life (t_1/2 = 2.8 min) in in vitro rat hepatic microsomes stability tests, an average inhibitor concentration of 390 µM in blood can be reached in mice even 6 h after a single i.p. dose of 200 µl per animal.

A cell-permeable triazolothienopyrimidine compound that acts as a reversible urea transporter B-selective inhibitor (IC50 = 10.3 and 25.1 nM against urea influx using human and mouse erythrocytes, respectively) by targeting a UT-B intracellular site in a urea-competitive manner, exhibiting little effect toward UT-A1, UT-A3, AQP1, CFTR, or TMEM16A channel activities. Shown to effectively decrease maximum urinary concentration and increase urination volume from antidiuretic dDAVP-treated wild-type, but not UT-B^-/-, mice (300 µg/300 µl/mouse i.p.) in vivo.

生物化学的／生理学的作用

Cell permeable: yes

Primary Target
urea transporter B

Reversible: yes

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

その他情報

Anderson, M.O., et al. 2012. J. Med. Chem.55, 5942.
Yao, C., et al. 2012. J. Am. Soc. Nephrol.23, 1210.

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 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable