P11149

• CAT Number: I045675
• CAS Number: 164724-79-2
• Molecular Formula: C27H34ClNO4
• Molecular Weight: 472.02
• Purity: ≥95%
• Synonyms: [(1S,12S,14R)-14-hydroxy-4-methyl-11-oxa-4-azatetracyclo[8.6.1.01,12.06,17]heptadeca-6(17),7,9,15-tetraen-9-yl] adamantane-1-carboxylate;hydrochloride
• InChI: InChI=1S/C27H33NO4.ClH/c1-28-7-6-27-5-4-20(29)11-22(27)32-24-21(3-2-19(15-28)23(24)27)31-25(30)26-12-16-8-17(13-26)10-18(9-16)14-26;/h2-5,16-18,20,22,29H,6-15H2,1H3;1H/t16?,17?,18?,20-,22-,26?,27-;/m0./s1
• InChIKey: NXIVVAIJLAXRRL-COWQPDHPSA-N
• SMILES: CN1CCC23C=CC(CC2OC4=C(C=CC(=C34)C1)OC(=O)C56CC7CC(C5)CC(C7)C6)O.Cl

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].

Reference

[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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