ProductDescription
LY-2811376isaorally-available,non-peptidicinhibitorofhBACE1withanIC50of239nM.SelectivityofLY-2811376forBACE1overBACE2wasfoundtobe10-fold,and50-foldorgreateroverrelatedaspartylproteasescathepsinD,pepsin,orrenin.[1]InAPP-overexpressinghumanembryonickidneycelllines,LY-2811376treatmentdecreasedAbsecretioninaconcentration-dependentfashion,withanEC50of~300nM.InprimaryneuronalculturesofPDAPPtransgenicmouse,AbsecretionwasmeasuredatanEC50of~100nM.
Invivo,LY2811376inhibitsBACE1activitybyconcomitantlyreducingC99andsAPPb,thetwoprimaryAPPcleavageproductsgeneratedbyBACE1.
Technicalinformation:
| ChemicalFormula: | C15H14F2N4S | |
| CAS#: | 1194044-20-6 | |
| MolecularWeight: | 320.36 | |
| Purity: | >98% | |
| Appearance: | White | |
| ChemicalName: | (S)-4-(2,4-difluoro-5-(pyrimidin-5-yl)phenyl)-4-methyl-5,6-dihydro-4H-1,3-thiazin-2-amine | |
| Solubility: | Upto50mMinDMSO | |
| Synonyms: | LY-2811376,LY2811376,LY2811376 |
ShippingCondition:Theproductisshippedinaglassvialatambienttemperature.
Storagecondition:Forlongershelflife,storesolidpowderat4oCdesiccated,orstoreDMSOsolutionat-20oC.
Reference:
| 1. | Mayetal.,Robustcentralreductionofamyloid-?inhumanswithanorallyavailable,non-peptidic?-secretaseinhibitor.J.Neurosci.,2011,31(46),16507-16516.PubmedID:22090477 |
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