PHA 568487
Based on 1 publication(s) in Google Scholar
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.
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- CAS. Nr.: 527680-57-5
- Formel: C20H24N2O7
- Molecular Weight:404.41
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Speicherung:
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Biologische Aktivität
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) PHA 568487
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Biologische Aktivität
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.
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.
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Animal Model:C57BL/6J male mice (10-12 weeks old)[2]
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Dosage:PHA 568487 (PHA; 0.4 and 0.8 mg/kg); Methyllycaconitine (MLA; 4 and 6 mg/kg)
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Administration:Injected intraperitoneally once on day 1, or twice on days 1 and 2, after pMCAO
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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.
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Animal Model:Adult male Sprague-Dawley rats (297 6±8.3 g)[4]
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Dosage:1.25 mg/kg
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Administration:I.p.;0.1 mL; treated daily
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Result:Showed a significant reduction of the cerebral infarct volumes and an improvement of the neurologic outcome.
Chemical Information
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CAS. Nr. 527680-57-5
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Molecular Weight 404.41
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Formel C20H24N2O7
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SMILES
OC(/C=C/C(O)=O)=O.O=C(C1=CC=C(OCCO2)C2=C1)N[C@@H]3C4CCN(CC4)C3
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
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Journal Impact Factor
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Most Recent
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Epilepsy Res
Long-term administration of EQU-001 (ivermectin) suppresses spasms in a rat model of infantile epileptic spasms syndrome. [Abstract]2026 Jan:219:107712. PMID: 41275582
Reinheit & Dokumentation
Verweise
[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]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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