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Urea Transporter B Inhibitor, UTBinh-14-Calbiochem

品牌
Sigma-Aldrich
货号
666125
包装型号
规格纯度
参考价格
2934.43 *本价格含增值税费
促销
数量
-+
产品介绍:

产品说明

一般描述

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 (t1/2 = 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.

包装

10 mg in Glass bottle
Packaged under inert gas

生化/生理作用

Cell permeable: yes
Primary Target
urea transporter B
Reversible: yes

警告

Toxicity: Standard Handling (A)

其他说明

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

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C20H17N5O2S3
分子量455.58

产品性质

质量水平100
测定≥98% (HPLC)
形式powder
manufacturer/tradenameCalbiochem®
储存条件OK to freeze
protect from light
颜色 white
溶解性DMSO: 100 mg/mL
运输ambient
储存温度2-8℃

安全信息

储存分类代码11 - Combustible Solids
WGKWGK 3
闪点(F)Not applicable
闪点(C)Not applicable

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