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表单
powder
质量水平
浓度
≥98 mg/mL (HPLC)
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear
储存温度
2-8°C
SMILES字符串
C12=C(N3CCOCC3)N=C(SC4=C5N=NN=C4N6CCNCC6)C5=C1CCCC2
InChI key
ZPVQONCMKZBGTB-UHFFFAOYSA-N
一般描述
UNC10201652 is a potent and substrate-dependent slow-binding inhibitor of bacterial β-glucuronidases (GUSs) in the gut. UNC10201652 appears to target a catalytic intermediate. It alleviates irinotecan-induced gut damage in mouse models of cancer.
生化/生理作用
potent and selective slow binding inhibitor microbiome β-glucuronidase enzyme
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
Samuel J Pellock et al.
ACS central science, 4(7), 868-879 (2018-08-01)
Microbial β-glucuronidases (GUSs) cause severe gut toxicities that limit the efficacy of cancer drugs and other therapeutics. Selective inhibitors of bacterial GUS have been shown to alleviate these side effects. Using structural and chemical biology, mass spectrometry, and cell-based assays
Kristen A Biernat et al.
Scientific reports, 9(1), 825-825 (2019-01-31)
Bacterial β-glucuronidase (GUS) enzymes cause drug toxicity by reversing Phase II glucuronidation in the gastrointestinal tract. While many human gut microbial GUS enzymes have been examined with model glucuronide substrates like p-nitrophenol-β-D-glucuronide (pNPG), the GUS orthologs that are most efficient
Aadra P Bhatt et al.
Proceedings of the National Academy of Sciences of the United States of America, 117(13), 7374-7381 (2020-03-15)
Irinotecan treats a range of solid tumors, but its effectiveness is severely limited by gastrointestinal (GI) tract toxicity caused by gut bacterial β-glucuronidase (GUS) enzymes. Targeted bacterial GUS inhibitors have been shown to partially alleviate irinotecan-induced GI tract damage and
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