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PHA 568487

SKU: orb1217928

Description

The quinuclidine PHA 568487 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.

Research Area

Metabolism Research

Images & Validation

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PHA 568487

Key Properties

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CAS Number527680-56-4
MW288.34
Purity>98% (HPLC)
FormulaC16H20N2O3
SMILESO=C(c(cc1)cc2c1OCCO2)N[C@@H]1C(CC2)CCN2C1
TargetAChR
SolubilityH2O:<40.44mg/ml (100mM); DMSO:<40.44mg/ml (100mM)

Bioactivity

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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. 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. 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. Animal model: C57BL/6J male mice (10-12 weeks old) with pMCAO. 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. 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.
In Vitro
PHA 568487, α-7 nAchR-specific agonist, prevents NF-κb activation in the cells. PHA 568487 treatment significantly reduces the expression of leukocyte infiltration molecules in MCAO rats and in endothelial cells after in vitro ischemia.

Storage & Handling

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StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

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Quick Database Links

Gene Symbol
AChR

Protocol Information

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$ 110.00
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$ 160.00
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$ 880.00
500 mg
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