278779-30-9 Usage
Uses
Different sources of media describe the Uses of 278779-30-9 differently. You can refer to the following data:
1. A novel nonsteroidal FXR nuclear receptor agonist
2. A novel nonsteroidal FXR nuclear receptor agonist.
3. GW4064 has been used:to investigate its ability to protect the livers of mice from lipopolysaccharide (LPS)-induced inflammation and apoptosisto examine its capability to inhibit mucosal injury in ileum caused by lipopolysaccharide (LPS)to treat ileal explants
General Description
GW4064 is a synthetic isoxazole, which is used to decipher the cellular and physiological functions of farnesoid X receptor (FXR). It is an estrogen receptor-related receptors (ERRs) agonist.
Biological Activity
Selective, non-steroidal farnesoid X receptor (FXR) agonist (EC 50 = 15 nM). Displays no activity at other nuclear receptors at concentrations up to 1 μ M. Improves hyperglycaemia and hyperlipidaemia in diabetic db/db mice.
Biochem/physiol Actions
GW4064 is a FXR agonist. GW4064 is a potent (EC50 = 15 nM), non-steroidal agonist of the orphan nuclear receptor FXR. It shows no activity on other nuclear receptors including RAR up to 1 mM. This is an important tool for the study of the involvment of FXR in a variety of biological activities.
references
[1] chiang pc, thompson dc, ghosh s, heitmeier mr. a formulation-enabled preclinical efficacy assessment of a farnesoid x receptor agonist, gw4064, in hamsters and cynomolgus monkeys. j pharm sci. 2011 nov;100(11):4722-33. [2] watanabe m, houten sm, wang l, moschetta a, mangelsdorf dj, heyman ra, moore dd, auwerx j. bile acids lower triglyceride levels via a pathway involving fxr, shp, and srebp-1c. j clin invest. 2004 may;113(10):1408-18.[3] li w, fu j, cheng f, zheng m, zhang j, liu g, tang y. unbinding pathways of gw4064 from human farnesoid x receptor as revealed by molecular dynamics simulations. j chem inf model. 2012 nov 26;52(11):3043-52.
Check Digit Verification of cas no
The CAS Registry Mumber 278779-30-9 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 2,7,8,7,7 and 9 respectively; the second part has 2 digits, 3 and 0 respectively.
Calculate Digit Verification of CAS Registry Number 278779-30:
(8*2)+(7*7)+(6*8)+(5*7)+(4*7)+(3*9)+(2*3)+(1*0)=209
209 % 10 = 9
So 278779-30-9 is a valid CAS Registry Number.
InChI:InChI=1/C28H22Cl3NO4/c1-16(2)27-21(26(32-36-27)25-22(29)7-4-8-23(25)30)15-35-20-12-11-18(24(31)14-20)10-9-17-5-3-6-19(13-17)28(33)34/h3-14,16H,15H2,1-2H3,(H,33,34)/b10-9+
278779-30-9Relevant articles and documents
Substituted isoxazole analogs of farnesoid X receptor (FXR) agonist GW4064
Bass, Jonathan Y.,Caldwell, Richard D.,Caravella, Justin A.,Chen, Lihong,Creech, Katrina L.,Deaton, David N.,Madauss, Kevin P.,Marr, Harry B.,McFadyen, Robert B.,Miller, Aaron B.,Parks, Derek J.,Todd, Dan,Williams, Shawn P.,Wisely, G. Bruce
experimental part, p. 2969 - 2973 (2010/01/16)
Starting from the known FXR agonist GW 4064 1a, a series of alternately 3,5-substituted isoxazoles was prepared. Several of these analogs were potent full FXR agonists. A subset of this series, with a tether between the isoxazole ring and the 3-position aryl substituent, were equipotent FXR agonists to GW 4064 1a, with the 2,6-dimethyl phenol analog 1t having greater FRET FXR potency than GW 4064 1a.
Identification of a chemical tool for the orphan nuclear receptor FXR
Maloney,Parks,Haffner,Fivush,Chandra,Plunket,Creech,Moore,Wilson,Lewis,Jones,Willson
, p. 2971 - 2974 (2007/10/03)
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