666125

Urea Transporter B Inhibitor, UTB_inh-14

• Sinônimo(s): 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
• Fórmula empírica (Notação de Hill): C₂₀H₁₇N₅O₂S₃
• Peso molecular: 455.58
• Código UNSPSC: 12352200
• NACRES: NA.28

Propriedades

• Ensaio: ≥98% (HPLC)
• Nível de qualidade: 100
• Formulário: powder
• fabricante/nome comercial: Calbiochem^®
• condição de armazenamento: OK to freeze; protect from light
• cor: white
• solubilidade: DMSO: 100 mg/mL
• Condições de expedição: ambient
• temperatura de armazenamento: 2-8°C

Descrição

Descrição geral

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.

Ações bioquímicas/fisiológicas

Cell permeable: yes

Primary Target
urea transporter B

Reversible: yes

Embalagem

Packaged under inert gas

Advertência

Toxicity: Standard Handling (A)

Outras notas

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

Informações legais

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

Informações de segurança

• Código de classe de armazenamento: 11 - Combustible Solids
• Classe de risco de água (WGK): WGK 3
• Ponto de fulgor (°F): Not applicable
• Ponto de fulgor (°C): Not applicable