BiologicalActivity
PotentLXRagonist(IC50valuesare24and179nMforLXRβandLXRα,respectively).ReducestotalserumcholesterolandLDLcholesterol,andinhibitslesiongrowthinmodelsofatherosclerosis.IncreasesABCA1andABCG1mRNAlevelsinratperipheralbloodcells.Orallybioavailable.
LicensingInformation
SoldforresearchpurposesunderagreementfromPfizerInc.
TechnicalData
| M.Wt | 422.78 |
| Formula | C21H12ClF5N2 |
| Storage | Storeat+4°C |
| Purity | ≥98%(HPLC) |
| CASNumber | 875787-07-8 |
| PubChemID | 16734800 |
| InChIKey | KYWWJENKIMRJBI-UHFFFAOYSA-N |
| Smiles | ClC1=CC(F)=CC=C1CN2N=C3C(C(F)(F)F)=CC=CC3=C2C4=CC=C(F)C=C4 |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
| Solvent | MaxConc.mg/mL | MaxConc.mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 42.28 | 100 | |
| ethanol | 42.28 | 100 |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight422.78.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 2.37mL | 11.83mL | 23.65mL |
| 5mM | 0.47mL | 2.37mL | 4.73mL |
| 10mM | 0.24mL | 1.18mL | 2.37mL |
| 50mM | 0.05mL | 0.24mL | 0.47mL |
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