574013-66-4 Usage
Description
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 (; EC50 = 80 nM). Fexaramine does not display activity at the following nuclear receptors: hRXRα, hPPARαγδ, mPXR, hPXR, hLXRα, hTRβ, hRARβ, mCAR, mERRγ, or hVDR.
Uses
Fexaramine has been used to study its action on RANKL (receptor activator of nuclear factor-κB ligand)-induced osteoclastogenesis in mouse model.
General Description
Fexaramine belongs to the nuclear hormone receptor family.
Biological Activity
Potent, selective farnesoid X receptor agonist (EC 50 = 25 nM). Displays no activity at hRXR α , hPPAR α , hPPAR γ , hPPAR δ , mPXR, hPXR, hLXR α , hTR β , hRAR β , mCAR, mERR γ and hVDR receptors.
Biochem/physiol Actions
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.
Check Digit Verification of cas no
The CAS Registry Mumber 574013-66-4 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 5,7,4,0,1 and 3 respectively; the second part has 2 digits, 6 and 6 respectively.
Calculate Digit Verification of CAS Registry Number 574013-66:
(8*5)+(7*7)+(6*4)+(5*0)+(4*1)+(3*3)+(2*6)+(1*6)=144
144 % 10 = 4
So 574013-66-4 is a valid CAS Registry Number.
574013-66-4Relevant articles and documents
NON-STEROIDAL FXR AGONISTS
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Page 12; 13; 34-36; Sheet 18, (2010/02/07)
ABSTRACT Potent non-steroidal farnesoid X receptor (FXR) agonists are N-aryl-N-arylmethyl amido and ureido compounds having the chemical structure represented by the following formula (I): INSERT FORMULA wherein E1 is (C1-C8)alkyl, cyclohexyl, 2-furyl, 3-