Fexaramine_product_DataBase

Bioactivity

Fexaramine is a potent and selective FXR agonist with an EC50 of 25 nM. Fexaramine has no activity against hRXRα, hPPARαγδ, mPXR, hPXR, hLXRα, hTRβ, hRARβ, mCAR, mERRγ, and hVDR receptors[1][2].

Invitro

Bile acid treatment is performed in HuTu-80 cells with Fexaramine (5, 25, and 50 μM) for 24 h. Fexaramine (50 μM) increases small heterodimer partner (SHP) transcript levels by 2.1-fold. The cells are treated with various concentrations of Fexaramine, and the endogenous secretin transcript levels are significantly reduced (33% in 50 μM Fexaramine). Fexaramine treatment also significantly suppresses secretin promoter activity by 32%[1].

In Vivo

Fexaramine treatment of DIO mice produces a striking metabolic profile that includes reduced weight gain, decreased inflammation, browning of WAT and increased insulin sensitization[3].

Name

Fexaramine

CAS

574013-66-4

Formula

C32H36N2O3

Molar Mass

496.64

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

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]. Michael Downes, et al. A chemical, genetic, and structural analysis of the nuclear bile acid receptor FXR. Mol Cell. 2003 Apr;11(4):1079-92. [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.

PeptideDB

Fexaramine

CAS: 574013-66-4 F: C32H36N2O3 W: 496.64