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Merck
CN

SML4267

MDMG-935P

≥98% (HPLC), powder, GO inhibitor

别名:

2-Hydroxy-5-(5-((prop-2-yn-1-ylamino)methyl)furan-2-yl)benzoic acid

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关于此项目

经验公式(希尔记法):
C15H13NO4
化学文摘社编号:
分子量:
271.27
Assay:
≥98% (HPLC)
Form:
powder
Quality level:
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产品名称

MDMG-935P, ≥98% (HPLC), powder, GO inhibitor

Quality Level

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear (warmed)

storage temp.

2-8°C

Application

MDMG-935P may be used for evaluating the expression of fatty acid oxidation (FAO) genes and inflammatory/fibrotic markers, and for assessing liver steatosis.

Biochem/physiol Actions

MDMG-935P is a potent dual, noncompetitive inhibitor of glycolateoxidase (GO) and lactate dehydrogenase A (LDHA), targeting catalytic bindingsites with an IC50 of 9 µM for hLDHA and demonstrating robust in vitro oxalatereduction. It selectively modulates key pathways involved in oxalateoverproduction and upregulates fatty acid oxidation genes, such as CPT1α,showing significant efficacy in reducing liver triglycerides, oxalate levels,and hepatic fibrosis in MASH mouse models at an oral dose of 10 mg/kg. Invitro, Agxt1−/− mouse hepatocytes are employed to model primary hyperoxaluria,and HEK-293 cells are used to assess cytotoxicity. With its favorable metabolicstability, minimal toxicity, anti-fibrotic properties, oral bioavailability, and enhanced efficacy, MDMG-935P is an invaluable tool for investigatinghyperoxaluria and metabolic liver diseases.

存储类别

11 - Combustible Solids

flash_point_f

Not applicable

flash_point_c

Not applicable

法规信息

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分析证书(COA)

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Maria Dolores Moya-Garzon et al.
European journal of medicinal chemistry, 237, 114396-114396 (2022-05-03)
The synthesis and biological evaluation of double glycolate oxidase/lactate dehydrogenase inhibitors containing a salicylic acid moiety is described. The target compounds are obtained in an easily scalable two-step synthetic procedure. These compounds showed low micromolar IC50 values against the two
Sandeep Das et al.
Nature metabolism, 6(10), 1939-1962 (2024-09-28)
The incidence of metabolic dysfunction-associated steatohepatitis (MASH) is on the rise, and with limited pharmacological therapy available, identification of new metabolic targets is urgently needed. Oxalate is a terminal metabolite produced from glyoxylate by hepatic lactate dehydrogenase (LDHA). The liver-specific

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