BiologicalActivity
Selective,orallyactivenon-steroidalagonistfortheliverXreceptor(LXR).Incell-basedreportergeneassays,actsasafullagonistofhLXRαandhLXRβ(EC50valuesare190and30nMrespectively).ReducesangiotensinII-mediatedincreasesinbloodpressure;up-regulatesABCA1geneexpressionandraisescirculatingHDLlevels.Displayspotentantiatherogenicactivityinmousemodelsofatherosclerosis.
LicensingInformation
SoldforresearchpurposesunderagreementfromGlaxoSmithKline
CompoundLibraries
GW3965hydrochlorideisalsoofferedaspartoftheTocriscreenPlus.FindoutmoreaboutcompoundlibrariesavailablefromTocris.
TechnicalData
| M.Wt | 618.51 |
| Formula | C33H31NO3ClF3.HCl |
| Storage | DesiccateatRT |
| Purity | ≥98%(HPLC) |
| CASNumber | 405911-17-3 |
| PubChemID | 16078973 |
| InChIKey | NMPUWJFHNOUNQU-UHFFFAOYSA-N |
| Smiles | Cl.OC(=O)CC1=CC=CC(OCCCN(CC(C2=CC=CC=C2)C2=CC=CC=C2)CC2=C(Cl)C(=CC=C2)C(F)(F)F)=C1 |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
| Solvent | MaxConc.mg/mL | MaxConc.mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 61.85 | 100 | |
| ethanol | 12.37 | 20 |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight618.51.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 1.62mL | 8.08mL | 16.17mL |
| 5mM | 0.32mL | 1.62mL | 3.23mL |
| 10mM | 0.16mL | 0.81mL | 1.62mL |
| 50mM | 0.03mL | 0.16mL | 0.32mL |
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