Fexaramine significantly enhanced osteoblastic differentiation through the upregulation of Runx2 and enhanced extracellular signal-regulated kinase (ERK) and β-catenin signaling. By mimicking this tissue-selective effect, the gut-restricted FXR agonist fexaramine (Fex) robustly induces enteric fibroblast growth factor 15 (FGF15), leading to alterations in BA composition, but does so without activating FXR target genes in the liver.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||10 mM in DMSO|
Positive regulation of osteogenesis by bile acid through FXR. J Bone Miner Res.
Cho SW, et al. J Bone Miner Res. 2013 Oct;28(10):2109-21.
Intestinal FXR agonism promotes adipose tissue browning and reduces obesity and insulin resistance.
Fang S, et al. Nat Med. 2015 Feb;21(2):159-65.
|Related Farnesoid X Receptor Products|
Cilofexor is a farnesoid X receptor (FXR) agonist.
WAY-362450 (XL335) is a potent, selective, and orally bioavailable FXR agonist with EC50 of 4 nM.
GW4064 is a selective, non-steroidal agonist of the orphan nuclear receptor FXR with EC50 of 15 nM.
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