P11149 |
| Catalog No.GC63134 |
P11149는 경쟁적인 BBB 투과성 약하게 경구 활성 및 선택적 AChE 억제제입니다.
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Cas No.: 164724-79-2
Sample solution is provided at 25 µL, 10mM.
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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.
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