
BiologicalActivity
ReversIBLe,competitiveinhibitorofsterolregulatoryelement-bindingprotein(SREBP)site1protease(IC50=0.175μM).Selectiveforsite1proteaseagainstapanelofserineproteases.InhibitsrateofcholesterolsynthesisinCHOcells(IC50=0.53μM).Alsodisplaysantiviralactivity.Cellpermeable.
LicensingInformation
SoldforresearchpurposesunderagreementfromPfizerInc.
CompoundLibraries
PF429242isalsoofferedaspartoftheTocriscreenPlus.FindoutmoreaboutcompoundlibrariesavailablefromTocris.
TechnicalData
M.Wt | 482.49 |
Formula | C25H35N3O2.2HCl |
Storage | DesiccateatRT |
Purity | ≥97%(HPLC) |
CASNumber | 947303-87-9 |
PubChemID | 90488837 |
InChIKey | GSUZWFZKTIOWTI-MQWQBNKOSA-N |
Smiles | O=C(C2=CC=C(CN(CC)CC)C=C2)N(CCC3=CC=CC=C3OC)[C@@H]1CCNC1.Cl.Cl |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
Solvent | MaxConc.mg/mL | MaxConc.mM | |
---|---|---|---|
Solubility | |||
DMSO | 24.12 | 50 | |
ethanol | 48.25 | 100 | |
water | 24.12 | 50 |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight482.49.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
---|---|---|---|
1mM | 2.07mL | 10.36mL | 20.73mL |
5mM | 0.41mL | 2.07mL | 4.15mL |
10mM | 0.21mL | 1.04mL | 2.07mL |
50mM | 0.04mL | 0.21mL | 0.41mL |