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经验公式(希尔记法):
C32H36N2O3
化学文摘社编号:
分子量:
496.64
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352116
MDL number:
产品名称
Fexaramine, ≥98% (HPLC)
InChI
1S/C32H36N2O3/c1-33(2)29-19-17-27(18-20-29)26-15-12-25(13-16-26)23-34(32(36)28-9-5-4-6-10-28)30-11-7-8-24(22-30)14-21-31(35)37-3/h7-8,11-22,28H,4-6,9-10,23H2,1-3H3/b21-14+
SMILES string
CN(C)C(C=C1)=CC=C1C2=CC=C(CN(C3=CC=CC(/C=C/C(OC)=O)=C3)C(C4CCCCC4)=O)C=C2
InChI key
VLQTUNDJHLEFEQ-KGENOOAVSA-N
assay
≥98% (HPLC)
form
powder
storage condition
desiccated
color
white to beige
solubility
DMSO: 10 mg/mL, clear
storage temp.
2-8°C
Quality Level
Application
Fexaramine has been used to study its action on RANKL (receptor activator of nuclear factor-κB ligand)-induced osteoclastogenesis in mouse model.
Biochem/physiol Actions
Fexaramine is a potent and selective agonist of the bile acid sensor farnesoid X receptor (FXR) in the gut with an EC50 of 25 nM and no activity found for other nuclear receptors. Fexaramine induces enteric fibroblast growth factor 15 (FGF15), causing alterations in bile acid composition without activating FXR target genes in the liver. In mouse studies, fexaramine enhanced thermogenesis and browning of white adipose tissue while reducing diet-induced weight gain, body-wide inflammation and hepatic glucose production. Fexaramine also improved insulin responsiveness.
Fexaramine is an agonist of the farnesoid X receptor (FXR).
Fexaramine might regulate lipid and glucose metabolism and can serve as a therapeutic target in the treatment of fatty liver disease, type 2 diabetes and obesity. Fexaramine might mediate cholesterol homeostasis and promotes osteoblast differentiation and suppresses differentiation of osteoclast.
General description
Fexaramine belongs to the nuclear hormone receptor family.
signalword
Warning
hcodes
Hazard Classifications
Acute Tox. 4 Oral - Aquatic Chronic 4
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
新产品
此项目有
Fexaramine Inhibits Receptor Activator of Nuclear Factor-?B Ligand-induced Osteoclast Formation via Nuclear Factor of Activated T Cells Signaling Pathways.
Zheng T, et al.
Journal of bone metabolism, 24(4), 207-215 (2017)
Farnesoid X receptor modulators (2011?2014): a patent review.
Sepe V, et al.
Expert Opinion on Therapeutic Patents, 25(8), 885-896 (2015)
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