PotentandselectiveDGAT-1inhibitor(IC50=19nM).Exhibits>1000-foldselectivityforDGAT-1overDGAT-2,andnosignificantactivityagainstarangeofotherenzymes,ionchannelsandreceptors.Reducesplasmatriglyceridelevelsinaratlipidchallengemodel.Orallybioavailable.
SoldforresearchpurposesunderagreementfromPfizerInc.
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.
Solvent | MaxConc.mg/mL | MaxConc.mM | |
---|---|---|---|
Solubility | |||
DMSO | 7.93 | 20 |
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 |