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666125 Urea Transporter B Inhibitor, UTBinh-14 - Calbiochem

666125
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Descripción

Replacement Information

Products

Número de referenciaEmbalaje Cant./Env.
666125-10MG Frasco de vidrio 10 mg
Description
OverviewA 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.
Catalogue Number666125
Brand Family Calbiochem®
Synonyms3-(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
References
ReferencesAnderson, M.O., et al. 2012. J. Med. Chem. 55, 5942.
Yao, C., et al. 2012. J. Am. Soc. Nephrol. 23, 1210.
Product Information
FormWhite powder
Hill FormulaC₂₀H₁₇N₅O₂S₃
Chemical formulaC₂₀H₁₇N₅O₂S₃
ReversibleY
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Primary Targeturea transporter B
Purity≥98% by HPLC
Physicochemical Information
Cell permeableY
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Standard Handling
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Número de referencia GTIN
666125-10MG 04055977183979

Documentation

Urea Transporter B Inhibitor, UTBinh-14 - Calbiochem Ficha datos de seguridad (MSDS)

Título

Ficha técnica de seguridad del material (MSDS) 

Urea Transporter B Inhibitor, UTBinh-14 - Calbiochem Certificados de análisis

CargoNúmero de lote
666125

Referencias bibliográficas

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

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision26-April-2013 JSW
Synonyms3-(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
DescriptionA 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.
FormWhite powder
Intert gas (Yes/No) Packaged under inert gas
Chemical formulaC₂₀H₁₇N₅O₂S₃
Structure formulaStructure formula
Purity≥98% by HPLC
SolubilityDMSO (100 mg/ml)
Storage Protect from light
+2°C to +8°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Toxicity Standard Handling
ReferencesAnderson, M.O., et al. 2012. J. Med. Chem. 55, 5942.
Yao, C., et al. 2012. J. Am. Soc. Nephrol. 23, 1210.