1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. nAChR
  3. PHA 568487 free base

PHA 568487 free base is a selective alpha 7 nicotinic acetylcholine receptor (α-7 nAchR) agonist. PHA 568487 free base reduces neuroinflammation.

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

PHA 568487 free base Chemical Structure

PHA 568487 free base Chemical Structure

CAS No. : 527680-56-4

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 105 In-stock
Solution
10 mM * 1 mL in DMSO USD 105 In-stock
Solid
1 mg USD 33 In-stock
5 mg USD 70 In-stock
10 mg USD 110 In-stock
50 mg USD 380 In-stock
100 mg USD 680 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

PHA 568487 free base is a selective alpha 7 nicotinic acetylcholine receptor (α-7 nAchR) agonist. PHA 568487 free base reduces neuroinflammation[1][2][3].

In Vitro

PHA 568487, α-7 nAchR-specific agonist, prevents NF-κb activation in the cells[2].
PHA 568487 treatment significantly reduces the expression of leukocyte infiltration molecules in MCAO rats and in endothelial cells after in vitro ischemia[3].

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

In Vivo

PHA 568487 treatment reduces mouse cognitive decline caused by aseptic bone fracture by promoting inflammation resolution. PHA 568487 (PHA; 0.8 mg/kg; injected intraperitoneally) reduces infarct volume and TUNEL positive neurons in the peri-infarct regions of permanent middle cerebral artery occlusion (pMCAO) and pMCAO+tibia fracture mice[2].
The role played by a7 receptors on neuroinflammation is supported by the decrease of [18F]DPA-714 binding in ischemic rats treated with the a7 agonist PHA 568487 at day 7 after MCAO[3].
PHA 568487-treated ischemic rats show a significant reduction of the cerebral infarct volumes and an improvement of the neurologic outcome compared with non-treated MCAO rats[3].

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

Animal Model: C57BL/6J male mice (10-12 weeks old) with pMCAO[2]
Dosage: 0.4 and 0.8 mg/kg
Administration: Injected intraperitoneally once on day 1, or twice on days 1 and 2, after pMCAO
Result: 0.8 mg/kg on days 1 and 2 after pMCAO yielded the best effect on infarct volume and behavior tests.
Animal Model: Adult male Sprague-Dawley rats[3]
Dosage: 1.25 mg/kg
Administration: Treated i.p. daily with 0.1 mL
Result: Showed a significant decrease of [18F]DPA-714 binding in the ischemic cerebral hemisphere in comparison to non-treated ischemic rats.
Molecular Weight

288.34

Formula

C16H20N2O3

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CC=C2C(OCCO2)=C1)N[C@@H]3C(CC4)CCN4C3

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 : 25 mg/mL (86.70 mM; ultrasonic and warming and adjust pH to 8 with HCl and heat to 80°C; 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 3.4681 mL 17.3406 mL 34.6813 mL
5 mM 0.6936 mL 3.4681 mL 6.9363 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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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: ≥ 2.08 mg/mL (7.21 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (7.21 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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+
%
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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).
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
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. 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 3.4681 mL 17.3406 mL 34.6813 mL 86.7032 mL
5 mM 0.6936 mL 3.4681 mL 6.9363 mL 17.3406 mL
10 mM 0.3468 mL 1.7341 mL 3.4681 mL 8.6703 mL
15 mM 0.2312 mL 1.1560 mL 2.3121 mL 5.7802 mL
20 mM 0.1734 mL 0.8670 mL 1.7341 mL 4.3352 mL
25 mM 0.1387 mL 0.6936 mL 1.3873 mL 3.4681 mL
30 mM 0.1156 mL 0.5780 mL 1.1560 mL 2.8901 mL
40 mM 0.0867 mL 0.4335 mL 0.8670 mL 2.1676 mL
50 mM 0.0694 mL 0.3468 mL 0.6936 mL 1.7341 mL
60 mM 0.0578 mL 0.2890 mL 0.5780 mL 1.4451 mL
80 mM 0.0434 mL 0.2168 mL 0.4335 mL 1.0838 mL
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PHA 568487 free base Related Classifications

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  • 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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PHA 568487 free base
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