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PD 144418 oxalate

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Catalog No. T39211Cas No. 1794760-28-3

PD 144418 oxalate is a highly potent and selective sigma 1 (σ1) receptor ligand with a Ki value of 0.08 nM for σ1 and 1377 nM for σ2, exhibiting negligible affinity for other receptors, ion channels, and enzymes, and demonstrating potential antipsychotic activity.

PD 144418 oxalate

PD 144418 oxalate

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Purity: 98.76%
Catalog No. T39211Cas No. 1794760-28-3
PD 144418 oxalate is a highly potent and selective sigma 1 (σ1) receptor ligand with a Ki value of 0.08 nM for σ1 and 1377 nM for σ2, exhibiting negligible affinity for other receptors, ion channels, and enzymes, and demonstrating potential antipsychotic activity.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$54-In Stock
5 mg$135-In Stock
10 mg$196-In Stock
25 mg$338-In Stock
50 mg$492-In Stock
100 mg$719-In Stock
200 mg$987-In Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:98.76%
Appearance:Solid
Color:Yellow
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Product Introduction

Bioactivity
Description
PD 144418 oxalate is a highly potent and selective sigma 1 (σ1) receptor ligand with a Ki value of 0.08 nM for σ1 and 1377 nM for σ2, exhibiting negligible affinity for other receptors, ion channels, and enzymes, and demonstrating potential antipsychotic activity.
Targets&IC50
σ1 receptor:0.08 nM (Ki), σ2 receptor:1377 nM (Ki)
In vitro
In vitro, PD 144418 counteracts the increase in cyclic GMP (cGMP) triggered by N-methyl-D-aspartate (NMDA) in rat cerebellar slices, without altering basal levels. This implies a significant role for σ1 sites in controlling actions induced by glutamine. Furthermore, PD 144418 enhances the reduction of 5-hydroxytryptophan induced by Haloperidol within the mesolimbic region, although it does not independently affect 5-HT and dopamine (DA) synthesis [1].
In vivo
Treatment with PD 144418 (10 mg/kg; intraperitoneal injection; male CD-1 mice) effectively antagonized Mescaline-induced scratching without affecting spontaneous motor activity, displaying an ED 50 of 7.0 mg/kg (i.p.). This outcome was observed in a study where male CD-1 mice were administered a single intraperitoneal dose of 10 mg/kg, resulting in the inhibition of scratching behaviors induced by Mescaline.
Chemical Properties
Molecular Weight372.42
FormulaC20H24N2O5
Cas No.1794760-28-3
SmilesO=C(O)C(=O)O.N=1OC(=CC1C=2C=CC(=CC2)C)C3=CCCN(C3)CCC
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: 10 mg/mL (26.85 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.6851 mL13.4257 mL26.8514 mL134.2570 mL
5 mM0.5370 mL2.6851 mL5.3703 mL26.8514 mL
10 mM0.2685 mL1.3426 mL2.6851 mL13.4257 mL
20 mM0.1343 mL0.6713 mL1.3426 mL6.7129 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:
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2 Enter the in vivo formulation:
% DMSO
%
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