347423

β-Glucuronidase Inhibitor

The β-Glucuronidase Inhibitor controls the biological activity of β-Glucuronidase.

• Sinonimo/i: β-Glucuronidase Inhibitor, 1-((6,8-Dimethyl-2-oxo-1,2-dihydroquinolin-3-yl)methyl)-3-(4-ethoxyphenyl)-1-(2-hydroxyethyl)thiourea
• Formula empirica (notazione di Hill): C₂₃H₂₇N₃O₃S
• Numero CAS: 484006-66-8
• Peso molecolare: 425.54
• Numero MDL: MFCD02747821
• Codice UNSPSC: 12352200
• NACRES: NA.28

Proprietà

• Livello qualitativo: 100
• Saggio: ≥99% (HPLC)
• Stato: solid
• Produttore/marchio commerciale: Calbiochem^®
• Condizioni di stoccaggio: OK to freeze; protect from light
• Colore: white
• Solubilità: DMSO: 50 mg/mL
• Condizioni di spedizione: ambient
• Temperatura di conservazione: 2-8°C
• Stringa SMILE: O=C(N1)C(CN(C(NC2=CC=C(C=C2)OCC)=S)CCO)=CC3=C1C(C)=CC(C)=C3

Descrizione

Descrizione generale

An orally bioavailable trisubstituted thiourea compound that acts as a potent, uncompetitive and reversible inhibitor of bacterial β-glucuronidase activity (IC₅₀ = 283 nM; k_cat/K_m = 0.0987 s^-1µM^-1; K_i = 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).

Confezionamento

Packaged under inert gas

Attenzione

Toxicity: Standard Handling (A)

Ricostituzione

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Altre note

Wallace, B.D., et al. 2010. Science330, 831.

Note legali

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

Informazioni sulla sicurezza

• Codice della classe di stoccaggio: 11 - Combustible Solids
• Classe di pericolosità dell'acqua (WGK): WGK 2
• Punto d’infiammabilità (°F): Not applicable
• Punto d’infiammabilità (°C): Not applicable