1. Neuronal Signaling
  2. Cholinesterase (ChE)
  3. P11149

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.

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P11149 Chemical Structure

P11149 Chemical Structure

CAS No. : 164724-79-2

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5 mg USD 450 In-stock
10 mg USD 800 In-stock
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  • References

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Description

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].

IC50 & Target

AChE

 

In Vivo

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

472.02

Formula

C27H34ClNO4

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C12C[C@H](C3)C[C@H](C[C@H]3C2)C1)OC4=CC=C5C6=C4O[C@]7([H])[C@@]6(CCN(C)C5)C=C[C@H](O)C7.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (211.86 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1186 mL 10.5928 mL 21.1855 mL
5 mM 0.4237 mL 2.1186 mL 4.2371 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 5 mg/mL (10.59 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 5 mg/mL (10.59 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.23%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1186 mL 10.5928 mL 21.1855 mL 52.9639 mL
5 mM 0.4237 mL 2.1186 mL 4.2371 mL 10.5928 mL
10 mM 0.2119 mL 1.0593 mL 2.1186 mL 5.2964 mL
15 mM 0.1412 mL 0.7062 mL 1.4124 mL 3.5309 mL
20 mM 0.1059 mL 0.5296 mL 1.0593 mL 2.6482 mL
25 mM 0.0847 mL 0.4237 mL 0.8474 mL 2.1186 mL
30 mM 0.0706 mL 0.3531 mL 0.7062 mL 1.7655 mL
40 mM 0.0530 mL 0.2648 mL 0.5296 mL 1.3241 mL
50 mM 0.0424 mL 0.2119 mL 0.4237 mL 1.0593 mL
60 mM 0.0353 mL 0.1765 mL 0.3531 mL 0.8827 mL
80 mM 0.0265 mL 0.1324 mL 0.2648 mL 0.6620 mL
100 mM 0.0212 mL 0.1059 mL 0.2119 mL 0.5296 mL
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P11149 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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P11149
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