A selective FXR agonist (EC50 = 25 nM) that demonstrates 100-fold increased affinity to FXR compared to endogenous bile acids and 3-fold increased potency compared to the high affinity FXR agonist GW 4064 (EC50 = 80 nM)

Fexaramine – 50 mg

Brand:
Cayman
CAS:
574013-66-4
Storage:
-20
UN-No:
Non-Hazardous - /

The farnesoid X receptor (FXR) is a nuclear receptor that acts as a bile acid sensor, protecting cells and organs against bile acid toxicity and coordinating cholesterol metabolism, lipid homeostasis, and absorption of dietary fats and vitamins. Fexaramine is an FXR agonist (EC50 = 25 nM) that demonstrates 100-fold increased affinity to FXR compared to endogenous bile acids and 3-fold increased potency compared to the high affinity FXR agonist GW 4064 (Item No. 10006611; EC50 = 80 nM).{28351} Fexaramine does not display activity at the following nuclear receptors: hRXRα, hPPARαγδ, mPXR, hPXR, hLXRα, hTRβ, hRARβ, mCAR, mERRγ, or hVDR.{28351}  

 

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Description

A selective FXR agonist (EC50 = 25 nM) that demonstrates 100-fold increased affinity to FXR compared to endogenous bile acids and 3-fold increased potency compared to the high affinity FXR agonist GW 4064 (EC50 = 80 nM)

Formal name: 3-[3-[(cyclohexylcarbonyl)[[4′-(dimethylamino)[1,1′-biphenyl]-4-yl]methyl]amino]phenyl]-2-propenoic acid, methyl ester

Synonyms: 

Molecular weight: 496.6

CAS: 574013-66-4

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Research Area|Endocrinology & Metabolism|Hormones & Receptors|FXRs & LXRs

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