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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-Farnesoid X Receptor (FXR)-INT-767
INT-767

Chemical Structure : INT-767

CAS No.: 1000403-03-1

INT-767 (INT767)

货号: PC-43034Not For Human Use, Lab Use Only.

INT-767 (INT767) is a potent, selective, dual farnesoid X receptor (FXR) and TGR5 agonist with EC50 of 30 and 630 nM, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    INT-767 (INT767) is a potent, selective, dual farnesoid X receptor (FXR) and TGR5 agonist with EC50 of 30 and 630 nM, respectively.
    INT-767 fails to activate 15 other nuclear receptors involved in metabolic pathways, and does not inhibit cytochrome P450 enzymes.
    INT-767 induces FXR-dependent lipid uptake by adipocytes and promotes TGR5-dependent glucagon-like peptide-1 (GLP-1) secretion by enteroendocrine cells.
    INT-767 markedly decreases cholesterol and triglyceride levels in diabetic db/db mice.

    物理化学性质&存储条件

    分子量 494.6601
    分子式 C25H43NaO6S
    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

    DMSO: ≥ 205.5 mg/mL

    Chemical Name/SMILES

    24-Norcholane-3,7,23-triol, 6-ethyl-, 23-(hydrogen sulfate), sodium salt (1:1), (3α,5β,6α,7α)-

    参考文献

    1. Rizzo G, et al. Mol Pharmacol. 2010 Oct;78(4):617-30.

    2. Baghdasaryan A, et al. Hepatology. 2011 Oct;54(4):1303-12.

    3. McMahan RH, et al. J Biol Chem. 2013 Apr 26;288(17):11761-70.

    4. Wang XX, et al. J Biol Chem. 2017 Jul 21;292(29):12018-12024.

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