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Merck
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重要文件

SML3236

Sigma-Aldrich

UNC10201652

≥98 mg/mL (HPLC)

同義詞:

4-(8-(piperazin-1-yl)-1,2,3,4-tetrahydro-[1,2,3]triazino[4′,5′:4,5]thieno[2,3-c]isoquinolin-5-yl)morpholine, 1,2,3,4-Tetrahydro-5-(4-morpholinyl)-8-(1-piperazinyl)[1,2,3]triazino[4′,5′:4,5]thieno[2,3-c]isoquinoline

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About This Item

經驗公式(希爾表示法):
C20H25N7OS
CAS號碼:
分子量::
411.52
分類程式碼代碼:
12352107
NACRES:
NA.77
暫時無法取得訂價和供貨情況

形狀

powder

品質等級

濃度

≥98 mg/mL (HPLC)

顏色

white to beige

溶解度

DMSO: 2 mg/mL, clear

儲存溫度

2-8°C

SMILES 字串

C12=C(N3CCOCC3)N=C(SC4=C5N=NN=C4N6CCNCC6)C5=C1CCCC2

InChI 密鑰

ZPVQONCMKZBGTB-UHFFFAOYSA-N

一般說明

UNC10201652 is a potent and substrate-dependent slow-binding inhibitor of bacterial β-glucuronidases (GUSs) in the gut.[1] 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

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable


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分析證明 (COA)

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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
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
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

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