ELN318463 racemate (C007B-353403)

ELN318463 racemate is the racemate of ELN318463. ELN318463 is an amyloid precursor protein (APP) selective γ-secretase inhibitor. ELN318463 shows differential inhibition of presenilin (PS1)- and PS2-comprised γ-secretase with EC 50 s of 12nM and 656 nM for PS1and PS2, respectively. ELN318463 is 51-fold more selective for PS1In 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.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 Aβ 1-40 and Aβ x-40 in BACE KO or wild-type BACE inhibitor treated mice has been reported . MCE has not independently confirmed the accuracy of these methods. They are for reference only.IC50& Target:γ-secretase.

Molecular Formula: C19H20BrClN2O3S

Molecular Weight: 471.80

PubChem CID: 18455200

Isomeric SMILES: C1CCNC(=O)C(C1)N(CC2=CC=C(C=C2)Br)S(=O)(=O)C3=CC=C(C=C3)Cl