cas 278779-30-9, GW 4064 | Articles data ｜lookchem

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278779-30-9

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Substituted isoxazole analogs of farnesoid X receptor (FXR) agonist GW4064
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.
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)

Assays for ligands for nuclear receptors
The present invention includes nuclear receptor heterodimer and nuclear receptor-coactivator pepetide assays for identifying ligands for nuclear receptors, utilizing scintillation proximity and fluorescence resonance energy transfer (FRET), and methods of using identified ligands.
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Page/Page column 16

(2010/11/30)

Identification of a chemical tool for the orphan nuclear receptor FXR
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Maloney,Parks,Haffner,Fivush,Chandra,Plunket,Creech,Moore,Wilson,Lewis,Jones,Willson
p. 2971 - 2974
(2007/10/03)

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Chemical Properties

Boiling Point: 702.054 °C at 760 mmHg
Flash Point:378.389 °C
Density: 1.367 g/cm³
Solubility:DMSO: soluble10mg/mL, clear
Storage Temp.:Desiccate at +4°C
Vapor Pressure: 0mmHg at 25°C
Refractive Index: 1.654
PKA: 4.13±0.10(Predicted)
PSA: 72.56000
LogP: 8.87280

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