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BMS-708163(Avagacestat)isapotentandselectiveinhibitorforgamma-secretase,especiallyatinhibitingcleavageofamyloidprecursorprotein(APP)toformamyloid-ß(Aß)(1-40)(IC50=0.3nM)andAß(1-42)(0.27nM).BMS-708163isNotchsparing,withmorethan100foldsmoreselectiveforAPPthanforNotchprotein(IC50of58nM).
BMS-708163isdevelopedfortreatingAlzheimersdisease(AD).OraladministrationofBMS-708163significantlyreducedAß(1-40)levelsforsustainedperiodsinbrain,plasma,andcerebrospinalfluidinratsanddogs[1].TheresultsofPhaseIIclinicaltrialinmild-to-moderateADpatientsdemonstratedacceptabletolerabilityatasingle-doserangeof0.3to800mgwithabiphasiceffectonplasmaAß(1-40)[2].
Technicalinformation:
| ChemicalFormula: | C20H17ClF4N4O4S | |
| CAS#: | 1146699-66-2 | |
| MolecularWeight: | 520.88 | |
| Purity: | >98% | |
| Appearance: | White | |
| ChemicalName: | (2R)-2-(N-(2-fluoro-4-(1,2,4-oxadiazol-3-yl)benzyl)-4-chlorophenylsulfonamido)-5,5,5-trifluoropentanamide | |
| Solubility: | Upto50mMinDMSO | |
| Synonyms: | BMS-708163,BMS708163,BMS708163,Avagacestat |
ShippingCondition:Theproductisshippedinaglassvialatambienttemperature.
Storagecondition:Forlongershelflife,storesolidpowderat4oCdesiccated,orstoreDMSOsolutionat-20oC.
Reference:
| 1. | Gillman,KW.,etal.DiscoveryandEvaluationofBMS-708163,aPotent,SelectiveandOrallyBioavailable?-SecretaseInhibitor.ACSMed.Chem.Lett.,2010,1(3):120124 |
| 2. | TongG.,etal.,Multicenter,randomized,double-blind,placebo-controlled,single-ascendingdosestudyoftheoral?-secretaseinhibitorBMS-708163(Avagacestat):tolerabilityprofile,pharmacokineticparameters,andpharmacodynamicMarkers.ClinTher.2012.34(3):654-67.PubmedID:22381714 |