P11149 是 Galanthamine 的一个衍生物，是有效的、竞争性的、弱透过血脑屏障的、口服活性的、选择性的 AChE 抑制剂，具有中枢胆碱能活性和安全性。P11149 抑制大鼠 BChE/AChE 的 IC50 值为 1.3 μM。P11149 用于阿尔兹海默症的研究。
货号:ajcx35082
CAS:164724-79-2
分子式:C27H34ClNO4
分子量：472.02
溶解度:DMSO : 100 mg/mL (211.86 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

P11149 is a competitive, BBB-penetarated weakly, orally active and selective inhibitor of AChE. P11149 exhibits an IC50 of 1.3 μM for rat BChE/AChE. P11149, a Galanthamine derivative, demonstrates central cholinergic activity, behavioral efficacy and safety. P11149 is used in the study for Alzheimer’s disease[1].

P11149 is a GAL analog that is rapidly hydrolyzed in vivo to yield the potent AChE inhibitor, 6-DMG[1].P11149 exhibits greater s.c. bioavailability than p.o. [1].Oral P11149 in mice produces Sal, Lac and tremors at doses similar to those in rats, whereas 6-DMG, P1 1012 and GAL produces Sal and Lac at doses lower than those in rats[1].P11149 exhibits T1/2(el) of 2.4 h and Cmax of 585 ng/mL in rat plasma[1].

[1]. G M Bores, et al. Pharmacological evaluation of novel Alzheimer’s disease therapeutics: acetylcholinesterase inhibitors related to galanthamine. J Pharmacol Exp Ther. 1996 May;277(2):728-38.