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β-Glucuronidase Inhibitor
An 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).
产品信息
Form White solid
Molar mass 425.5
Protect from Light 是的
Packaged under inert gas 是的
Purity ≥99% by HPLC
Solubility DMSO
Chemical formula C23H27N3O3S
商店和运输信息
Storage +2°C to +8°C
Ship Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
Standard Handling |