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PHA 568487 free base

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Catalog No. T23146Cas No. 527680-56-4
Alias PHA 568487

The quinuclidine PHA 568487 free base is an agonist of the alpha 7 nicotinic acetylcholine receptor that was designed to mitigate the bioactivation associated with the core scaffold and subsequently remove associated liabilities with in vivo tolerability.

PHA 568487 free base

PHA 568487 free base

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Purity: 99.74%
Catalog No. T23146Alias PHA 568487Cas No. 527680-56-4
The quinuclidine PHA 568487 free base is an agonist of the alpha 7 nicotinic acetylcholine receptor that was designed to mitigate the bioactivation associated with the core scaffold and subsequently remove associated liabilities with in vivo tolerability.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
10 mg$37In StockIn Stock
25 mg$68In StockIn Stock
50 mg$132In StockIn Stock
100 mg$237In StockIn Stock
200 mg$331-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:99.74%
Appearance:Solid
Color:White
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Product Introduction

PHA 568487 free base AI Summary
PHA 568487 free base exhibits potent agonist activity at the rat alpha7 nicotinic acetylcholine receptor (nAChR) expressed in GH4C1 cells, with an EC50 value of 36.2 nM and an Emax value of 96.0% relative to nicotine. It also demonstrates antiviral activity by inhibiting SARS-CoV-2 induced cytotoxicity in both Caco-2 and VERO-6 cells, showing varying inhibition rates and concentrations. Specifically, it inhibited SARS-CoV-2 cytotoxicity at 10 µM after 48 hours, with inhibition percentages of -3.54% in Caco-2 cells and -0.04% in VERO-6 cells. Additionally, PHA 568487 free base moderately inhibits the SARS-CoV-2 3CL-Pro protease by approximately 9.983% at a concentration of 20 µM. Furthermore, it shows inhibitory activity against human HDAC6, with greater efficacy observed using a commercial peptide substrate compared to a custom peptide substrate..
Note: Summary generated by AI. Data source: ChEMBL
Bioactivity
Description
The quinuclidine PHA 568487 free base is an agonist of the alpha 7 nicotinic acetylcholine receptor that was designed to mitigate the bioactivation associated with the core scaffold and subsequently remove associated liabilities with in vivo tolerability.
SynonymsPHA 568487
Chemical Properties
Molecular Weight288.34
FormulaC16H20N2O3
Cas No.527680-56-4
SmilesO=C(N[C@H]1CN2CCC1CC2)c1ccc2OCCOc2c1
Relative Density.no data available
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: 30 mg/mL (104.04 mM), Sonication is recommended.
H2O: < 40.44 mg/mL (100 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (6.94 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
H2O/DMSO
1mg5mg10mg50mg
1 mM3.4681 mL17.3406 mL34.6813 mL173.4064 mL
5 mM0.6936 mL3.4681 mL6.9363 mL34.6813 mL
10 mM0.3468 mL1.7341 mL3.4681 mL17.3406 mL
20 mM0.1734 mL0.8670 mL1.7341 mL8.6703 mL
50 mM0.0694 mL0.3468 mL0.6936 mL3.4681 mL
100 mM0.0347 mL0.1734 mL0.3468 mL1.7341 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

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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

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