
ELN318463 racemate
CAS No. 851599-82-1
ELN318463 racemate( ELN 318463 racemate | ELN318463 (racemate) )
Catalog No. M26194 CAS No. 851599-82-1
ELN 318463 shows differential inhibition of presenilin (PS1)- and PS2-comprised γ-secretase with EC50s of 12nM and 656 nM for PS1and PS2, respectively.
Purity : >98% (HPLC)






Size | Price / USD | Stock | Quantity |
5MG | 619 | Get Quote |
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10MG | 972 | Get Quote |
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25MG | 1431 | Get Quote |
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50MG | 1953 | Get Quote |
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100MG | 2628 | Get Quote |
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200MG | Get Quote | Get Quote |
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500MG | Get Quote | Get Quote |
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1G | Get Quote | Get Quote |
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Biological Information
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Product NameELN318463 racemate
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NoteResearch use only, not for human use.
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Brief DescriptionELN 318463 shows differential inhibition of presenilin (PS1)- and PS2-comprised γ-secretase with EC50s of 12nM and 656 nM for PS1and PS2, respectively.
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DescriptionELN 318463 shows differential inhibition of presenilin (PS1)- and PS2-comprised γ-secretase with EC50s of 12nM and 656 nM for PS1and PS2, respectively. ELN318463 is 51-fold more selective for PS1. ELN 318463 racemate is the racemate of ELN 318463. ELN 318463 is an amyloid precursor protein (APP) selective γ-secretase inhibitor.(In Vitro):ELN318463 shows differential inhibition of presenilin (PS1)- and PS2-comprised γ-secretase with EC50s of 12nM and 656 nM for PS1and PS2, respectively.(In Vivo):Brain levels of ELN318463 (30 mg/kg) are 0.754 μM in FVB brains and 0.69 μM, and of ELN318463(100 mg/kg) are 2.7 μM in FVB brains and 1.87 μM in PDAPP brains.
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In VitroELN318463 behaves as a classic γ-secretase inhibitor, demonstrates 75- to 120-fold selectivity for inhibiting Aβ production compared with Notch signaling in cells, and displaces an active site directed inhibitor at very high concentrations only in the presence of substrate.
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In VivoBrain levels of ELN318463 at 30 mg/kg are 0.754 μM in FVB brains and 0.69 μM in PDAPP brains, and at 100 mg/kg dose the levels were 2.7 μM in FVB brains and 1.87 μM in PDAPP brains. Discordance between Aβ1-40 and Aβx-40 in BACE KO or wild-type BACE inhibitor treated mice has been reported.
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SynonymsELN 318463 racemate | ELN318463 (racemate)
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PathwayOthers
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TargetOther Targets
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RecptorTopoisomerase I
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Research Area——
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Indication——
Chemical Information
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CAS Number851599-82-1
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Formula Weight471.79
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Molecular FormulaC19H20BrClN2O3S
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Purity>98% (HPLC)
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Solubility——
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SMILESClc1ccc(cc1)S(=O)(=O)N(Cc1ccc(Br)cc1)C1CCCCNC1=O
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Chemical Name——
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1.Ogitani Y, et al. DS-8201a, A Novel HER2-Targeting ADC with a Novel DNA Topoisomerase I Inhibitor, Demonstrates a Promising Antitumor Efficacy with Differentiation from T-DM1. Clin Cancer Res. 2016 Oct 15;22(20):5097-5108.
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