β-Glucuronidase-IN-1 是强效的,选择性,非竞争性和具有口服活性的 E. coli β-葡萄糖醛酸酶 (β-glucuronidase) 抑制剂,针对 E. coli β-葡萄糖醛酸酶的 IC50 和 Ki 值分别为 283 nM 和 164 nM。
生物活性
β-Glucuronidase-IN-1 is a potent, selective, uncompetitive, and orally active E. coli bacterial β-glucuronidase inhibitor, exhibiting an IC 50 and a K i of 283 nM and 164 nM, respectively.
性状
Solid
IC50 & Target[1][2]
IC50: 283 nM (E. coli β-glucuronidase)Ki: 164 nM (E. coli β-glucuronidase)
体外研究(In Vitro)
β-Glucuronidase-IN-1 (Inhibitor 1) (0.01-100 μM) inhibits E. coli β-glucuronidase activity as a dose-dependent manner and exhibits an IC50 and a Ki value with 283 nM and 164 nM, respectively.β-Glucuronidase-IN-1 (100 μM; 24-72 hours) maintains potent efficacy in living bacterial cells (EC50=17.7 nM), it does not affect bacterial cell growth under aerobic or anaerobic conditions or killing mammalian epithelial cells. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
β-Glucuronidase-IN-1 (oral gavage; 10 μg; twice per day; 11 days) protects the mouse GI epithelium from CPT-11–induced damage and protects the glandular structure of CPT-11-treated intestinal tissues. has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Wallace BD, et al. Alleviating cancer drug toxicity by inhibiting a bacterial enzyme.Science. 2010 Nov 5;330(6005):831-5.
溶解度数据
In Vitro: DMSO : 100 mg/mL (235.00 mM; Need ultrasonic)配制储备液