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Cellagentech/BMS-708163 (Avagacestat) | γ-secretase inhibitor/C3670-5/5 mg (powder)

价格
¥3380.00
货号:C3670-5
浏览量:127
品牌:Cellagen
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商品描述
ProductDescription

BMS-708163(Avagacestat)isapotentandselectiveinhibitorforgamma-secretase,especiallyatinhibitingcleavageofamyloidprecursorprotein(APP)toformamyloid-ß(Aß)(1-40)(IC50=0.3nM)andAß(1-42)(0.27nM).BMS-708163is“Notchsparing”,withmorethan100foldsmoreselectiveforAPPthanforNotchprotein(IC50of58nM).

BMS-708163isdevelopedfortreatingAlzheimer’sdisease(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):120–124
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

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