| Size | Price | Stock | Qty |
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| 5mg |
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| ln Vitro |
A α-7 nAchR-specific agonist, PHA 568487, inhibits NF-κb activation in cells[2]. Following in vitro ischemia, PHA 568487 treatment dramatically lowers the expression of leukocyte infiltration molecules in MCAO rats and endothelial cells[3].
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| ln Vivo |
Through the promotion of inflammation resolution, PHA 568487 therapy mitigates the cognitive deterioration in mice resulting from aseptic bone fractures. Intraperitoneally administered PHA 568487 (PHA; 0.8 mg/kg) decreases TUNEL positive neurons and infarct volume in the peri-infarct areas of permanent middle cerebral artery occlusion (pMCAO) and pMCAO+tibia fracture mice[2]. The decrease of [18F]DPA-714 binding in ischemic rats treated with the a7 agonist PHA 568487 at day 7 after MCAO[3] provides evidence for the role a7 receptors play in neuroinflammation. When compared to non-treated MCAO rats, ischemic rats treated with PHA 568487 exhibit a significant reduction in cerebral infarct volumes and an improvement in the neurologic outcome[3].
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| Animal Protocol |
Animal/Disease Models: C57BL/6J male mice (10-12 weeks old) with pMCAO[2]
Doses: 0.4 and 0.8 mg/kg Route of Administration: Injected intraperitoneally (ip) once on day 1, or twice on days 1 and 2, after pMCAO Experimental Results: 0.8 mg/kg on days 1 and 2 after pMCAO yielded the best effect on infarct volume and behavior tests. Animal/Disease Models: Adult male SD (Sprague-Dawley) rats[3] Doses: 1.25 mg/kg Route of Administration: Treated ip daily with 0.1 mL Experimental Results: demonstrated a significant decrease of [18F]DPA-714 binding in the ischemic cerebral hemisphere in comparison to non-treated ischemic rats. |
| 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.
[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. [3]. 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. |
| Molecular Formula |
C16H20N2O3
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|---|---|
| Molecular Weight |
288.34
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| CAS # |
527680-56-4
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| Related CAS # |
PHA 568487;527680-57-5
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| SMILES |
O=C(N[C@@H]1C2CCN(CC2)C1)C1=CC2OCCOC=2C=C1.OC(/C=C/C(O)=O)=O
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 25 mg/mL (86.70 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.21 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (7.21 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (7.21 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.3468 mL | 1.7341 mL | 3.4681 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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