Fexaramine

• CAT Number: I004141
• CAS Number: 574013-66-4
• Molecular Formula: C32H36N2O3
• Molecular Weight: 496.60
• Purity: ≥95%
• Synonyms: (E)-methyl 3-(3-(N-((4/’-(dimethylamino)-[1,1/’-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)phenyl)acrylate
• Target: LXR
• Solubility: 10 mM in DMSO
• Storage: Desiccate at +4C
• IUPAC Name: methyl (E)-3-[3-[cyclohexanecarbonyl-[[4-[4-(dimethylamino)phenyl]phenyl]methyl]amino]phenyl]prop-2-enoate
• InChI: 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+
• InChIKey: VLQTUNDJHLEFEQ-KGENOOAVSA-N
• SMILES: CN(C)C1=CC=C(C=C1)C2=CC=C(C=C2)CN(C3=CC=CC(=C3)/C=C/C(=O)OC)C(=O)C4CCCCC4

Fexaramine（Cat No.:I004141）is a synthetic small-molecule agonist of the farnesoid X receptor (FXR), a key regulator of bile acid homeostasis and metabolism. Unlike traditional FXR agonists, Fexaramine remains confined to the gut, activating FXR locally without systemic absorption. This unique mechanism offers potential for treating metabolic disorders like obesity, type 2 diabetes, and non-alcoholic fatty liver disease (NAFLD) by modulating bile acid metabolism, improving insulin sensitivity, and reducing inflammation. Fexaramine’s localized action minimizes side effects, making it a promising candidate for gut-targeted therapies in metabolic health management.

Reference

[1]. Lam IP, et al. Bile acids inhibit duodenal secretin expression via orphan nuclear receptor small heterodimer partner (SHP). Am J Physiol Gastrointest Liver Physiol. 2009 Jul;297(1):G90-7.
[2]. Cho SW, et al. Positive regulation of osteogenesis by bile acid through FXR. J Bone Miner Res. 2013 Oct;28(10):2109-21.
[3]. Fang S, et al. Intestinal FXR agonism promotes adipose tissue browning and reduces obesity and insulin resistance. Nat Med. 2015 Feb;21(2):159-65.