PHA 568487

Cat. No.: HY-107666: FAQs
Data Sheet Handling Instructions

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PHA 568487 a selective agonist of alpha-7 nicotinic acetylcholine receptor (α-7 nAchR).PHA 568487 reduces neuroinflammation and oxidative stress. PHA-568487 has rapid brain penetration.

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

PHA 568487 Chemical Structure

CAS No. : 527680-57-5

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PHA 568487 free base In-stock

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Purity & Documentation
References
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Description

PHA 568487 a selective agonist of alpha-7 nicotinic acetylcholine receptor (α-7 nAchR)^[1]^[2].PHA 568487 reduces neuroinflammation and oxidative stress^[2]. PHA-568487 has rapid brain penetration^[3].

In Vitro

PHA 568487 increases anti-oxidant gene expression and decreases oxidative stress and phosphorylation of NF-κb p65. Methyllycaconitine (MLA) has the opposite effects^[2].
PHA increases anti-oxidant genes and NADPH oxidase expression associated with decreased phosphorylation of NF-kB p65 in microglia/macrophages^[3].

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

In Vivo

PHA 568487 attenuates neuronal injury and behavioral dysfunction in mice with ischemic stroke only and ischemic stroke plus tibia fracture^[2].
PHA 568487 (1.25 mg/kg; i.p.; treated daily)-treated ischemic rats shows a significant reduction of the cerebral infarct volumes and an improvement of the neurologic outcome^[4].

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)^[2]
Dosage:	PHA 568487 (PHA; 0.4 and 0.8 mg/kg); Methyllycaconitine (MLA; 4 and 6 mg/kg)
Administration:	Injected intraperitoneally once on day 1, or twice on days 1 and 2, after pMCAO
Result:	Injection of PHA (0.8 mg/kg) and MLA (6 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 (297 6±8.3 g)^[4]
Dosage:	1.25 mg/kg
Administration:	I.p.;0.1 mL; treated daily
Result:	Showed a significant reduction of the cerebral infarct volumes and an improvement of the neurologic outcome.

Molecular Weight

404.41

Formula

C₂₀H₂₄N₂O₇

CAS No.

527680-57-5

SMILES

OC(/C=C/C(O)=O)=O.O=C(C1=CC=C(OCCO2)C2=C1)N[C@@H]3C4CCN(CC4)C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility

In Vitro:

DMSO : 250 mg/mL (618.18 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	2.4727 mL	12.3637 mL	24.7274 mL
5 mM	0.4945 mL	2.4727 mL	4.9455 mL
10 mM	0.2473 mL	1.2364 mL	2.4727 mL

View the Complete Stock Solution Preparation Table

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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 (5.14 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
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 (5.14 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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (5.14 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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).

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

Handling Instructions (2659 KB)

References

[1]. F Barclay Shilliday, et al. Multiple species metabolism of PHA-568487, a selective alpha 7 nicotinic acetylcholine receptor agonist. Drug Metab Lett. 2010 Aug;4(3):162-72. [Content Brief]

[2]. Zhenying Han, et al. Alpha-7 nicotinic acetylcholine receptor agonist treatment reduces neuroinflammation, oxidative stress, and brain injury in mice with ischemic stroke and bone fracture. J Neurochem. 2014 Nov;131(4):498-508. [Content Brief]

[3]. Dingquan Zou, et al.Activation of Alpha-7 Nicotinic Acetylcholine Receptor Reduces Brain Edema in Mice with Ischemic Stroke and Bone Fracture. Mol Neurobiol. 2017 Dec;54(10):8278-8286. [Content Brief]

[4]. Lorena Colás, et al. In vivo imaging of Α7 nicotinic receptors as a novel method to monitor neuroinflammation after cerebral ischemia. Glia. 2018 Aug;66(8):1611-1624. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.4727 mL	12.3637 mL	24.7274 mL	61.8185 mL
	5 mM	0.4945 mL	2.4727 mL	4.9455 mL	12.3637 mL
	10 mM	0.2473 mL	1.2364 mL	2.4727 mL	6.1818 mL
	15 mM	0.1648 mL	0.8242 mL	1.6485 mL	4.1212 mL
	20 mM	0.1236 mL	0.6182 mL	1.2364 mL	3.0909 mL
	25 mM	0.0989 mL	0.4945 mL	0.9891 mL	2.4727 mL
	30 mM	0.0824 mL	0.4121 mL	0.8242 mL	2.0606 mL
	40 mM	0.0618 mL	0.3091 mL	0.6182 mL	1.5455 mL
	50 mM	0.0495 mL	0.2473 mL	0.4945 mL	1.2364 mL
	60 mM	0.0412 mL	0.2061 mL	0.4121 mL	1.0303 mL
	80 mM	0.0309 mL	0.1545 mL	0.3091 mL	0.7727 mL
	100 mM	0.0247 mL	0.1236 mL	0.2473 mL	0.6182 mL

PHA 568487 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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