BiologicalActivity
Potentandselectivediacylglycerolacyltransferase(DGAT-1)inhibitor(IC50=0.6nM).ExhibitsselectivityforDGAT-1overDGAT-2,Kv11.1(hERG)andcytochromeP450enzymes.Suppressestriacylglyceride(TAG)plasmaexcursionandadiposetissueTAGsynthesisinrats.Reducesbodyweightofdiet-inducedobeserats.Cellpermeableandorallybioavailable.
LicensingInformation
SoldwiththepermissionofAstraZenecaUKLtd.
CompoundLibraries
AZD3988isalsoofferedaspartoftheTocriscreenPlus.FindoutmoreaboutcompoundlibrariesavailablefromTocris.
TechnicalData
| M.Wt | 456.44 |
| Formula | C23H22F2N4O4 |
| Storage | Storeat+4°C |
| Purity | ≥98%(HPLC) |
| CASNumber | 892489-52-0 |
| PubChemID | 11676786 |
| InChIKey | ZGBGPEDJXCYQPH-UHFFFAOYSA-N |
| Smiles | O=C(NC3=CC=[C@@]([C@H]4CC[C@H](CC(O)=O)CC4)C=C3)C1=NN=C(NC2=CC(F)=C(F)C=C2)O1 |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
| Solvent | MaxConc.mg/mL | MaxConc.mM | |
|---|---|---|---|
| Solubility | |||
| 1eq.NaOH | 4.56 | 10mMwithgentlewarming | |
| DMSO | 45.64 | 100 |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight456.44.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 2.19mL | 10.95mL | 21.91mL |
| 5mM | 0.44mL | 2.19mL | 4.38mL |
| 10mM | 0.22mL | 1.1mL | 2.19mL |
| 50mM | 0.04mL | 0.22mL | 0.44mL |
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