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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-Farnesoid X Receptor (FXR)-Altenusin
Altenusin

Chemical Structure : Altenusin

CAS No.: 31186-12-6

Altenusin (2076A)

货号: PC-26301Not For Human Use, Lab Use Only.

Altenusin (2076A) is a nonsteroidal fungal metabolite and potent, selective agonist of Farnesoid X receptor (FXR) with EC50 of 3.2 uM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

Altenusin (2076A) is a nonsteroidal fungal metabolite and potent, selective agonist of Farnesoid X receptor (FXR) with EC50 of 3.2 uM.
Altenusin (2076A) shows little to no activity on 14 other receptors at 30 uM.
Altenusin (2076A) dose-dependently induces the expression of small heterodimer partner, bile salt export pump, and scavenger receptor class B1, three known FXR target genes, and suppresses the expression of cholesterol-7α-hydroxylase, a gene negatively regulated by FXR, in hepatocytes isolated from WT mice, but not in hepatocytes isolated from FXR KO mice.
Altenusin (2076A) binds to the LBD of FXR to activate FXR.
Altenusin (2076A) treatment (5, 10, 30 mg/kg, i.p.) leads to metabolic benefits in chow-fed mice, inhibits HFD-induced obesity.

物理化学性质&存储条件

分子量 290.27
分子式 C15H14O6
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

3,4',5'-Trihydroxy-5-methoxy-2'-methyl-[1,1'-biphenyl]-2-carboxylic acid

参考文献

1. Zheng Z, et al. Mol Pharmacol. 2017 Oct;92(4):425-436.

2. Nakanishi S, et al. Biosci Biotechnol Biochem 59:1333–1335.

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