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P11149

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Catalog No. T38005Cas No. 164724-79-2

P11149, a derivative of Galanthamine, acts as a competitive, orally active, and selective AChE inhibitor with the ability to weakly penetrate the blood-brain barrier (BBB). It demonstrates selective inhibition, exhibiting an IC50 of 1.3 μM for rat BChE/AChE, and shows central cholinergic activity, behavioral efficacy, and safety. P11149 is utilized in Alzheimer's disease research[1].

P11149

P11149

Copy Product Info
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Catalog No. T38005Cas No. 164724-79-2
P11149, a derivative of Galanthamine, acts as a competitive, orally active, and selective AChE inhibitor with the ability to weakly penetrate the blood-brain barrier (BBB). It demonstrates selective inhibition, exhibiting an IC50 of 1.3 μM for rat BChE/AChE, and shows central cholinergic activity, behavioral efficacy, and safety. P11149 is utilized in Alzheimer's disease research[1].
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
25 mg$1,3108-10 weeks8-10 weeks
50 mg$1,7108-10 weeks8-10 weeks
100 mg$2,5908-10 weeks8-10 weeks
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Product Introduction

Bioactivity
Description
P11149, a derivative of Galanthamine, acts as a competitive, orally active, and selective AChE inhibitor with the ability to weakly penetrate the blood-brain barrier (BBB). It demonstrates selective inhibition, exhibiting an IC50 of 1.3 μM for rat BChE/AChE, and shows central cholinergic activity, behavioral efficacy, and safety. P11149 is utilized in Alzheimer's disease research[1].
Targets&IC50
BChE/AChE (rat):1.3 μM (IC50)
In vivo
P11149 is a GAL analog that, upon rapid in vivo hydrolyzation, produces 6-DMG, a potent AChE inhibitor. It demonstrates superior subcutaneous (s.c.) bioavailability compared to oral (p.o.) administration. In mice, oral doses of P11149 induce salivation (Sal), lacrimation (Lac), and tremors at levels comparable to those observed in rats. Notably, 6-DMG, P1 1012, and GAL trigger Sal and Lac at lower doses in rats. Moreover, P11149 has a half-life (T1/2(el)) of 2.4 hours and reaches a maximum concentration (Cmax) of 585 ng/mL in rat plasma.
Chemical Properties
Molecular Weight472.02
FormulaC27H34ClNO4
Cas No.164724-79-2
SmilesCl.CN1CC[C@@]23C=C[C@H](O)C[C@@H]2Oc2c3c(C1)ccc2OC(=O)C12CC3CC(CC(C3)C1)C2
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 100 mg/mL (211.86 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween-80+45% Saline: 5 mg/mL (10.59 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.1186 mL10.5928 mL21.1855 mL105.9277 mL
5 mM0.4237 mL2.1186 mL4.2371 mL21.1855 mL
10 mM0.2119 mL1.0593 mL2.1186 mL10.5928 mL
20 mM0.1059 mL0.5296 mL1.0593 mL5.2964 mL
50 mM0.0424 mL0.2119 mL0.4237 mL2.1186 mL
100 mM0.0212 mL0.1059 mL0.2119 mL1.0593 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

Keywords

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