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

PHA 568487 

Cat. No.: HY-107666
Handling Instructions

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

PHA 568487 Chemical Structure

CAS No. : 527680-57-5

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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.
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)

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
*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: 2.08 mg/mL (5.14 mM); Suspended solution; Need ultrasonic

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.08 mg/mL (5.14 mM); Clear solution

*All of the co-solvents are available by MedChemExpress (MCE).
Purity & Documentation
References
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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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Product Name:
PHA 568487
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HY-107666
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