Elenbecestat

Research use only, not for human use.

Elenbecestat is an effective oral bioutilization and CNS penetrating ACE-1 inhibitor for the treatment of Alzheimer's disease.

Elenbecestat is an effective oral bioutilization and CNS penetrating ACE-1 inhibitor for the treatment of Alzheimer's disease.(In Vitro):Elenbecestat (E2609) is a potent BACE1 inhibitor with an IC50 of ~7 nmol/L in cell-based assay.Elenbecestat has been shown to reduce Ab production in the plasma, brain, and cerebrospinal fluid (CSF) of rodents.(In Vivo):Elenbecestat (E2609; 0.3-30 mg/kg; p.o.) potently inhibits Ab1-40 and Ab1-42 production in the plasma and CSF of non-human primates.Elenbecestat displays the plasma half-life of 12-16 hours after once daily dosing.

Elenbecestat (E2609) is a potent BACE1 inhibitor with an IC50 of ~7 nmol/L in cell-based assay.Elenbecestat has been shown to reduce Ab production in the plasma, brain, and cerebrospinal fluid (CSF) of rodents.

Elenbecestat (E2609; 0.3-30 mg/kg; p.o.) potently inhibits Ab1-40 and Ab1-42 production in the plasma and CSF of non-human primates.Elenbecestat displays the plasma half-life of 12-16 hours after once daily dosing. Animal Model:Cynomolgus monkeys (Pharmacokinetic analysis)Dosage:0.3 mg/kg; 1 mg/kg; 3 mg/kg; 30 mg/kg Administration:Oral administration Result:Potently inhibits Ab1-40 and Ab1-42 production in the plasma and CSF.

E2609

Metabolic Enzyme/Protease

BACE

BACE1

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1388651-30-6

437.44

C19H18F3N5O2S

>98% (HPLC)

DMSO:250 mg/mL (571.51 mM)

C[C@H]1OC[C@]2(c(cc(cc3)NC(c4ncc(C(F)F)nc4)=O)c3F)N=C(N)SC[C@H]12

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(-20℃)

With Ice Pack

≥ 2 years