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GW4064isapotent,orally-available,non-steroidal,isoxazole-basedagonistofFXRwithanEC50of15nM.InaFisherratmodel,GW4064wasfoundtolowerserumtriglyceridelevelsinadose-dependentmannerandanED50of20mg/kg.(1)
InC57BL/6mice,GW4064hasbeenshowntostimulateplasmacorticosteronelevels,thussuggestingaroleinthemodulationofadrenalcholesterolmetabolismandglucocorticoidsynthesis.(2)
FollowupSARstudieshaveledtoequipotentFXRanalogsofGW4064withimproveddevelopabilityparameters,includingreducedtoxicityandcholestasis.(3)
Technicalinformation:
| ChemicalFormula: | C28H22Cl3NO4 | |
| CAS#: | 278779-30-9 | |
| MolecularWeight: | 542.84 | |
| Purity: | >98% | |
| Appearance: | white | |
| ChemicalName: | (E)-3-(2-chloro-4-((3-(2,6-dichlorophenyl)-5-isopropylisoxazol-4-yl)methoxy)styryl)benzoicacid | |
| Solubility: | Upto100mMinDMSO | |
| Synonyms: | GW4064,GW-4064,GW4064 |
ShippingCondition:Theproductisshippedinaglassvialatambienttemperature.
Storagecondition:Forlongershelflife,storesolidpowderat4oCdesiccated,orstoreDMSOsolutionat-20oC.
Reference:
| 1. | Maloneyetal.,IdentificationofaChemicalToolfortheOrphanNuclearReceptorFXR.J.Med.Chem.2000,43(16),2971-2974.PubmedID:10956205 |
| 2. | Hoekstraetal.,FXRagonistGW4064increasesplasmaglucocorticoidlevelsinC57BL/6mice.Mol.Cell.Endocrinol.2012,362,69-75.PubmedID:22643070 |
| 3. | Akwabi-Ameyawetal.,ConformationallyconstrainedfarnesoidXreceptor(FXR)agonists:Naphthoicacid-basedanalogsofGW4064.Bioorg.Med.Chem.Lett.2008,18,4339-4343.PubmedID:18621523 |