BiologicalActivity
PotentandselectiveDGAT-1inhibitor(IC50=19nM).Exhibits>1000-foldselectivityforDGAT-1overDGAT-2,andnosignificantactivityagainstarangeofotherenzymes,ionchannelsandreceptors.Reducesplasmatriglyceridelevelsinaratlipidchallengemodel.Orallybioavailable.
LicensingInformation
SoldforresearchpurposesunderagreementfromPfizerInc.
TechnicalData
| M.Wt | 396.44 |
| Formula | C21H24N4O4 |
| Storage | Storeat+4°C |
| Purity | ≥98%(HPLC) |
| CASNumber | 1109276-89-2 |
| PubChemID | 46926360 |
| InChIKey | GEVVQZHMFVFGLN-UHFFFAOYSA-N |
| Smiles | O=C1N(C2=CC=C([C@@H]3CC[C@@H](CC(O)=O)CC3)C=C2)CCOC4=NC=NC(N)=C41 |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
| Solvent | MaxConc.mg/mL | MaxConc.mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 7.93 | 20 |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight396.44.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 2.52mL | 12.61mL | 25.22mL |
| 5mM | 0.5mL | 2.52mL | 5.04mL |
| 10mM | 0.25mL | 1.26mL | 2.52mL |
| 50mM | 0.05mL | 0.25mL | 0.5mL |
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