An inhibitor of BACE1 (Ki = 26.1 nM); binds selectively to BACE1 over BACE2 (Ki = 372.4 nM); inhibits hERG potassium channels (IC50 = 4.8 μM); decreases Aβ secretion from mouse Neuro2a neuroblastoma cells and primary neurons (IC50s = 32.2 and 50.9 nM

AZD3839 – 5 mg

Brand:
Cayman
CAS:
1227163-84-9
Storage:
-20
UN-No:
Non-Hazardous - /

AZD3839 is an inhibitor of beta-secretase 1 (BACE1).{48539,48540} It selectively binds to BACE1 over BACE2 (Kis = 26.1 and 372.4 nM, respectively, for the human enzymes).{48539} It also inhibits human ether-a-go-go-related gene (hERG) potassium channels expressed in CHO cells (IC50 = 4.8 μM).{48540} AZD3839 decreases amyloid-β (Aβ) secretion from mouse Neuro2a neuroblastoma cells and primary neurons (IC50s = 32.2 and 50.9 nM, respectively).{48539} It dose- and time-dependently decreases Aβ levels in the plasma and brain of mice and guinea pigs. AZD3839 also decreases Aβ in the cerebrospinal fluid (CSF) of cynomolgus monkeys when administered at a dose of 20 μmol/kg.  

 

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SKU: 28388 - 5 mg Category:

Description

An inhibitor of BACE1 (Ki = 26.1 nM); binds selectively to BACE1 over BACE2 (Ki = 372.4 nM); inhibits hERG potassium channels (IC50 = 4.8 μM); decreases Aβ secretion from mouse Neuro2a neuroblastoma cells and primary neurons (IC50s = 32.2 and 50.9 nM, respectively); dose- and time-dependently decreases Aβ levels in the plasma and brain of mice and guinea pigs; decreases Aβ levels in the CSF of cynomolgus monkeys at 20 μmol/kg

Formal name: (1S)-1-[2-(difluoromethyl)-4-pyridinyl]-4-fluoro-1-[3-(5-pyrimidinyl)phenyl]-1H-isoindol-3-amine

Synonyms: 

Molecular weight: 431.4

CAS: 1227163-84-9

Purity: ≥98%

Formulation: A solid

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