1. Neuronal Signaling
  2. AChE
  3. P11149

P11149 

Cat. No.: HY-105327
Handling Instructions

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.

For research use only. We do not sell to patients.

P11149 Chemical Structure

P11149 Chemical Structure

CAS No. : 164724-79-2

Size Price Stock Quantity
5 mg USD 450 In-stock
Estimated Time of Arrival: December 31
10 mg USD 800 In-stock
Estimated Time of Arrival: December 31
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100 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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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

IC50: 1.3 μM (rat BChE/AChE)[1].

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].

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

Molecular Weight

472.02

Formula

C₂₇H₃₄ClNO₄

CAS No.

164724-79-2

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (211.86 mM; Need ultrasonic)

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
10 mM 0.2119 mL 1.0593 mL 2.1186 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 2.

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

    Solubility: ≥ 5.75 mg/mL (12.18 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
References
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  • Molarity Calculator

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This equation is commonly abbreviated as: C1V1 = C2V2

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Keywords:

P11149P 11149P-11149AChEAcetylcholinesteraseAlzheimer'sdiseaseBChEcholinesteraseGAL6-DMGInhibitorinhibitorinhibit

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P11149
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HY-105327
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