您的位置：首页 > 半岛bd体育手机客户端 中心 > Urea Transporter B Inhibitor, UTB
inh-14-Calbiochem
Urea Transporter B Inhibitor, UTBinh-14-Calbiochem
半岛bd体育手机客户端 别名
Urea Transporter B Inhibitor, UTBinh-14-Calbiochem
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
基本信息
| Empirical Formula【经验(实验)分子式】 |
C
20H
17N
5O
2S
3
|
| Molecular weight |
455.58
|
| General description【一般描述】 |
A cell-permeable triazolothienopyrimidine compound that acts as a reversible urea transporter B (UT-B)-selective inhibitor (IC
50= 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 ?M inhibitor treatment). Shown to effectively decrease maximum urinary concentration (2.3- and 3.7-fold of basal [urea], respectively, with or without inhibitor; 300 ?g/300 ?l/mouse i.p.) and increase urination volume (236 vs.109 ?l/4h, respectively, with or without inhibitor) from antidiuretic dDAVP- (1 ?g/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 vitrorat hepatic microsomes stability tests, an average inhibitor concentration of 390 ?M in blood can be reached in mice even 6 h after a single i.p. dose of 200 ?l per animal.
A cell-permeable triazolothienopyrimidine compound that acts as a reversible urea transporter B-selective inhibitor (IC 50= 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 ?g/300 ?l/mouse i.p.) in vivo. |
| Biochem/physiol Actions【生化/生理作用】 |
Cell permeable: yes
Primary Target urea transporter B Reversible: yes |
| Warning【警告】 |
Toxicity: Standard Handling (A)
|
| Other Notes【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. |
| Legal Information【法律信息】 |
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
|
半岛bd体育手机客户端 性质
| Quality Level【质量水平】 |
100
|
| Assay【测定】 |
≥98% (HPLC)
|
| form【形式】 |
powder
|
| manufacturer/tradename |
Calbiochem
?
|
| storage condition【储存条件】 |
OK to freeze
protect from light |
| color【颜色】 |
white
|
| solubility【溶解性】 |
DMSO: 100 mg/mL
|
| shipped in【运输】 |
ambient
|
| storage temp.【储存温度】 |
2-8℃
|
| 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 3
|
