AChE-IN-21

Names

[ CAS No. ]:
2413656-04-7

[ Name ]:
AChE-IN-21

Biological Activity

[Description]:

AChE-IN-21 (Compound I-8) is a potent, selective and orally active AChE inhibitor with an IC50 of 2.66 nM. AChE-IN-21 displays excellent BBB permeability in vitro[1].

[Related Catalog]:

Research Areas >> Neurological Disease
Signaling Pathways >> Neuronal Signaling >> AChE

[Target]

EeAChE:2.66 nM (IC50)

RatBuChE:19.10 μM (IC50)


[In Vitro]

AChE-IN-21 (Compound I-8) binds to both the catalytic active site and peripheral anionic site of AChE[1].

[In Vivo]

AChE-IN-21 (Compound I-8) (0-25 mg/kg; i.g.; once a day for 7 consecutive days) significantly reverses scopolamine-induced memory deficit in mice[1]. Animal Model: Kunming mice at body weight of 18–22 g (male and female in half)[1] Dosage: 1.0, 5.0 and 25.0 mg/kg Administration: Intragastric administration, once a day for 7 consecutive days Result: Obviously blocked scopolamine (2 mg/kg, i.p.)-induced memory deficit.

[References]

[1]. Luo L, et al. Design, synthesis and evaluation of phthalide alkyl tertiary amine derivatives as promising acetylcholinesterase inhibitors with high potency and selectivity against Alzheimer's disease. Bioorg Med Chem. 2020 Apr 15;28(8):115400.

Chemical & Physical Properties

[ Molecular Formula ]:
C24H29NO4

[ Molecular Weight ]:
395.49

Related Compounds