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| 100mg | ||
| 250mg | ||
| 500mg | ||
| Other Sizes |
| ln Vitro |
PHA 568487 reduces oxidative stress and phosphorylation of NF-κb p65 while increasing the expression of antioxidant genes. The effects of methyllycaconitine (MLA) are the opposite[2]. PHA raises the expression of NADPH oxidase and antioxidant genes, which are linked to a decrease in NF-kB p65 phosphorylation in macrophages and microglia[3].
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| ln Vivo |
PHA 568487 reduces behavioral dysfunction and neuronal damage in mice that have both ischemic stroke and stroke with a fractured tibia[2]. When administered intraperitoneally (1.25 mg/kg; treated daily), PHA 568487 significantly reduces the volumes of brain infarcts and improves the neurologic outcome in ischemic rats[4].
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| Animal Protocol |
Animal/Disease Models: C57BL/6J male mice (10-12 weeks old)[2]
Doses: PHA 568487 (PHA; 0.4 and 0.8 mg/kg); Methyllycaconitine (MLA; 4 and 6 mg/kg) Route of Administration: Injected intraperitoneally (ip) once on day 1, or twice on days 1 and 2, after pMCAO Experimental Results: 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/Disease Models: Adult male SD (Sprague-Dawley) rats (297 6±8.3 g)[4] Doses: 1.25 mg/kg Route of Administration: Ip;0.1 mL; treated daily Experimental Results: demonstrated a significant reduction of the cerebral infarct volumes and an improvement of the neurologic outcome. |
| 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]. 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. [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. |
| Molecular Formula |
C20H24N2O7
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|---|---|
| Molecular Weight |
404.41
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| CAS # |
527680-57-5
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| Related CAS # |
PHA 568487 free base;527680-56-4
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| SMILES |
OC(/C=C/C(=O)O)=O.O=C(C1=CC=C2OCCOC2=C1)NC1CN2CCC1CC2
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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: 250 mg/mL (618.18 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.08 mg/mL (5.14 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
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 (5.14 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 (5.14 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 | 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 |
*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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