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Merck
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주요 문서

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SML3236

Sigma-Aldrich

UNC10201652

≥98 mg/mL (HPLC)

동의어(들):

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

실험식(Hill 표기법):
C20H25N7OS
CAS Number:
372495-52-8
Molecular Weight:
411.52
UNSPSC 코드:
12352107
NACRES:
NA.77

양식

powder

Quality Level

100

농도

≥98 mg/mL (HPLC)

색상

white to beige

solubility

DMSO: 2 mg/mL, clear

저장 온도

2-8°C

SMILES string

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

InChI key

ZPVQONCMKZBGTB-UHFFFAOYSA-N

일반 설명

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.

생화학적/생리학적 작용

potent and selective slow binding inhibitor microbiome β-glucuronidase enzyme

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable

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시험 성적서(COA)

Lot/Batch Number

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문서 라이브러리 방문

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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