CNP-520

Research use only, not for human use.

CNP-520 (CNP520) is a novel potent, selective BACE1 inhibitor (pKa=7.2) for treatment of Alzheimer's disease.

CNP-520 (CNP520) is a novel potent, selective BACE1 inhibitor (pKa=7.2) for treatment of Alzheimer's disease, reduces brain and cerebrospinal fluid (CSF) Aβ in rats and dogs, and Aβ plaque deposition in APP-transgenic mice.Alzheimer's Disease Phase 3 Clinical.

Umibecestat (CNP520) is a potent BACE-1 inhibitor that is selective for BACE-1 over other human pepsin-like aspartic proteases, including BACE-2 and cathepsin D.

Umibecestat (CNP520) (1.5-51.3 mg/kg; given by oral gavage; 72 hours) shows a dose-dependent effects on Aβ40 and a long duration of action in both rat brain and CSF.Umibecestat (CNP520) (3.1 mg/kg; oral administration; 7 days) shows a > 75% reduction on Aβ40 and Aβ42 in CSF after dosing and returns slowly to baseline over the next 7 days. Animal Model:Male rats (3-4 months old) Dosage:1.5 mg/kg (3 μM/kg)-51.3 mg/kg (100 μM/kg) Administration:Given by oral gavage; 72 hours Result:Reduced 89.3±4.5% Aβ40 at the highest dose in brain tissue, and 50% lowering of rat brain Aβ40 (ED50) was 2.4±0.31 mg/kg. Reduced ~50% Aβ40 at a single oral 30 μM/kg (15.4 mg/kg) dose after 24 hours in both rat brain and CSF.Animal Model:3-month-old beagle dogs Dosage:3.1 mg/kg (6 μM/kg) Administration:Oral administration; 7 days Result:Both Aβ40 and Aβ42 concentrations in CSF showed a > 75% reduction at 12-48 h after dosing and returned slowly to baseline over the next 7 days.

CNP520

Metabolic Enzyme/Protease

BACE

BACE

Neurological Disease

Alzheimer Disease

1387560-01-1

513.801

C19H15ClF7N5O2

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (194.63 mM)

CC1(COC(C(=N1)N)(C)C(F)(F)F)C2=C(C=CC(=N2)NC(=O)C3=C(C=C(C=N3)C(F)(F)F)Cl)F

N-(6-((3R,6R)-5-amino-3,6-dimethyl-6-(trifluoromethyl)-3,6-dihydro-2H-1,4-oxazin-3-yl)-5-fluoropyridin-2-yl)-3-chloro-5-(trifluoromethyl)picolinamide

(-20℃)

With Ice Pack

≥ 2 years