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)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
5MG 619 Get Quote
10MG 972 Get Quote
25MG 1431 Get Quote
50MG 1953 Get Quote
100MG 2628 Get Quote
200MG Get Quote Get Quote
500MG Get Quote Get Quote
1G Get Quote Get Quote

Biological Information

  • Product Name
    ELN318463 racemate
  • Note
    Research use only, not for human use.
  • Brief Description
    ELN 318463 shows differential inhibition of presenilin (PS1)- and PS2-comprised γ-secretase with EC50s of 12nM and 656 nM for PS1and PS2, respectively.
  • Description
    ELN 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.
  • In Vitro
    ELN318463 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.
  • In Vivo
    Brain 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.
  • Synonyms
    ELN 318463 racemate | ELN318463 (racemate)
  • Pathway
    Others
  • Target
    Other Targets
  • Recptor
    Topoisomerase I
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    851599-82-1
  • Formula Weight
    471.79
  • Molecular Formula
    C19H20BrClN2O3S
  • Purity
    >98% (HPLC)
  • Solubility
    ——
  • SMILES
    Clc1ccc(cc1)S(=O)(=O)N(Cc1ccc(Br)cc1)C1CCCCNC1=O
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • 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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