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347423 β-Glucuronidase Inhibitor - Calbiochem

347423
Purchase on Sigma-Aldrich

Panoramica

Replacement Information

Tabella delle specifiche principali

Empirical Formula
C₂₃H₂₇N₃O₃S

Products

Numero di catalogoConfezionamento Qtà/conf
347423-10MG Bottiglia di vetro 10 mg
Description
OverviewAn orally bioavailable trisubstituted thiourea compound that acts as a potent, uncompetitive and reversible inhibitor of bacterial β-glucuronidase activity (IC50 = 283 nM; kcat/Km = 0.0987 s-1µM-1; Ki = 164 nM in vitro assays against E coli β-glucuronidase; EC50 = 17.7 nM in β-glucuronidase expressing HB101 cells) with excellent selectivity over mammalian β-glucuronidases. Shown to directly target the 17-residue (360-376) loop structure that protects the active site of E coli β-glucuronidase and alter its conformation. Displays negligible cytotoxicity toward both bacterial and mammalian epithelial cells (>> 100 µM for HCT116, Caco-2 and CMT93 colon cancer cells) and offers protection against CPT-11 (50 mg/kg, i.p., s.i.d. for 9 days)-induced toxicity in mice (10 µg, p.o., b.i.d).
Catalogue Number347423
Brand Family Calbiochem®
Synonyms1-((6,8-Dimethyl-2-oxo-1,2-dihydroquinolin-3-yl)methyl)-3-(4-ethoxyphenyl)-1-(2-hydroxyethyl)thiourea
References
ReferencesWallace, B.D., et al. 2010. Science 330, 831.
Product Information
FormWhite solid
Hill FormulaC₂₃H₂₇N₃O₃S
Chemical formulaC₂₃H₂₇N₃O₃S
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Purity≥99% by HPLC
Physicochemical Information
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
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

Documentation

β-Glucuronidase Inhibitor - Calbiochem MSDS

Titolo

Scheda di sicurezza (MSDS) 

β-Glucuronidase Inhibitor - Calbiochem Certificati d'Analisi

TitoloNumero di lotto
347423

Riferimenti bibliografici

Panoramica delle referenze
Wallace, B.D., et al. 2010. Science 330, 831.
Scheda tecnica

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.

Revision10-August-2012 JSW
Synonyms1-((6,8-Dimethyl-2-oxo-1,2-dihydroquinolin-3-yl)methyl)-3-(4-ethoxyphenyl)-1-(2-hydroxyethyl)thiourea
DescriptionAn orally bioavailable trisubstituted thiourea compound that acts as a potent, uncompetitive and reversible inhibitor of bacterial β-glucuronidase activity (IC50 = 283 nM; kcat/Km = 0.0987 s-1µM-1; Ki = 164 nM in vitro assays against E coli β-glucuronidase; EC50 = 17.7 nM in β-glucuronidase expressing HB101 cells) with excellent selectivity over mammalian β-glucuronidases. Shown to directly target the 17-residue (360-376) loop structure that protects the active site of E coli β-glucuronidase and alter its conformation. Displays negligible cytotoxicity toward both bacterial and mammalian epithelial cells (>> 100 µM for HCT116, Caco-2 and CMT93 colon cancer cells) and offers protection against CPT-11 (50 mg/kg, i.p., s.i.d. for 9 days)-induced toxicity in mice (10 µg, p.o., b.i.d).
FormWhite solid
Intert gas (Yes/No) Packaged under inert gas
Chemical formulaC₂₃H₂₇N₃O₃S
Structure formulaStructure formula
Purity≥99% by HPLC
SolubilityDMSO (50 mg/ml)
Storage +2°C to +8°C
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.
Toxicity Standard Handling
ReferencesWallace, B.D., et al. 2010. Science 330, 831.