P11149
目录号: PL01521 纯度: ≥99%
CAS No. :164724-79-2
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中文名称
P11149
英文名称
P11149
英文别名
Tricyclo[3.3.1.13,7]decane-1-carboxylicacid,(4aS,6R,8aS)-4a,5,9,10,11,12-hexahydro-6-hydroxy-11-methyl-6H-benzofuro[3a,3,2-ef][2]benzazepin-3-ylester, hydrochloride (1:1);Tricyclo[3.3.1.13,7]decane-1-carboxylicacid,(4aS,6R,8aS)-4a,5,9,10,11,12-hexahydro-6-hydroxy-11-methyl-6H-benzofuro[3a,3,2-ef;Galanthamine,O-demethyl-, 6-tricyclo[3.3.1.13,7]decane-1-carboxylate, hydrochloride;O-Demethylgalanthamine6-(adamantane-1-carboxylate), hydrochloride;P 11149;Tricyclo[3.3.1.13,7]decane-1-carboxylic acid,(4aS,6R,8aS)-4a,5,9,10,11,12-hexahydro-6-hydroxy-11-methyl-6H-benzofuro[3a,3,2-ef][2]benzazepin-3-ylester, hydrochloride (9CI);Tricyclo[3.3.1.13,7]decane-1-carboxylic acid,4a,5,9,10,11,12-hexahydro-6-hydroxy-11-methyl-6H-benzofuro[;P11149
Cas No.
164724-79-2
分子式
C27H34ClNO4
分子量
472.02
包装储存
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
产品详情
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。
生物活性
P11149 is a competitive, BBB-penetarated weakly, orally active and selective inhibitor of AChE. P11149 exhibits an IC 50 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 Alzheimers disease.
性状
Solid
IC50 & Target[1][2]
IC50: 1.3 μM (rat BChE/AChE).
体内研究(In Vivo)
P11149 is a GAL analog that is rapidly hydrolyzed in vivo to yield the potent AChE inhibitor, 6-DMG.
P11149 exhibits greater s.c. bioavailability than p.o. .
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.
P11149 exhibits T 1/2 (el) of 2.4 h and C max of 585 ng/mL in rat plasma.
has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献
[1]. G M Bores, et al. Pharmacological evaluation of novel Alzheimers disease therapeutics: acetylcholinesterase inhibitors related to galanthamine. J Pharmacol Exp Ther. 1996 May;277(2):728-38.
溶解度数据
In Vitro: DMSO : 100 mg/mL (211.86 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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