1. Neuronal Signaling
  2. Beta-secretase
  3. Umibecestat

Umibecestat (Synonyms: CNP520)

Cat. No.: HY-119689
Handling Instructions

Umibecestat (CNP520) is a beta-site amyloid precursor protein cleaving enzyme-1 (BACE-1) inhibitor with IC50s of 11 nM and 10 nM for human BACE-1 and mouse BACE-1, respectively.

For research use only. We do not sell to patients.

Umibecestat Chemical Structure

Umibecestat Chemical Structure

CAS No. : 1387560-01-1

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Description

Umibecestat (CNP520) is a beta-site amyloid precursor protein cleaving enzyme-1 (BACE-1) inhibitor with IC50s of 11 nM and 10 nM for human BACE-1 and mouse BACE-1, respectively[1].

IC50 & Target

IC50: 11 nM (human BACE-1), 10 nM (mouse BACE-1)[1]

In Vitro

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[1].

In Vivo

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[1].
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[1].

Animal Model: Male rats (3-4 months old)[1]
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[1]
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.
Clinical Trial
Molecular Weight

513.80

Formula

C₁₉H₁₅ClF₇N₅O₂

CAS No.

1387560-01-1

SMILES

O=C(NC1=NC([[email protected]@]2(CO[[email protected]](C)(C(N)=N2)C(F)(F)F)C)=C(C=C1)F)C3=NC=C(C=C3Cl)C(F)(F)F

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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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