
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 |
![]() ![]() |
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 NameELN318463 racemate
-
NoteResearch use only, not for human use.
-
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.
-
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.
-
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.
-
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.
-
SynonymsELN 318463 racemate | ELN318463 (racemate)
-
PathwayOthers
-
TargetOther Targets
-
RecptorTopoisomerase I
-
Research Area——
-
Indication——
Chemical Information
-
CAS Number851599-82-1
-
Formula Weight471.79
-
Molecular FormulaC19H20BrClN2O3S
-
Purity>98% (HPLC)
-
Solubility——
-
SMILESClc1ccc(cc1)S(=O)(=O)N(Cc1ccc(Br)cc1)C1CCCCNC1=O
-
Chemical Name——
Shipping & Storage Information
-
Storage(-20℃)
-
ShippingWith 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.
molnova catalog



related products
-
β-Caryophyllene
β-Caryophyllene is a CB2 receptor agonist.
-
Tilomisole
Tilomisole (Wy 18251) is an orally available benzimidazole thiazole with anti-inflammatory activity and immunomodulatory activity.Tilomisole is used in the study of cancer and inflammation.
-
HET0016
HET0016 is a potent and selective 20-HETE synthase inhibitor (IC50s: 17.7 nM, 12.1 nM, and 20.6 nM for recombinant CYP4A1-, CYP4A2-, and CYP4A3-catalyzed 20-HETE synthesis) and a selective CYP450 inhibitor, shown to inhibit angiogenesis and tumor growth.