Molecular structure of PHA 568487, CAS Number: 527680-56-4
PHA 568487 (CAS 527680-56-4)
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Alternate Names:
N-(3R)-1-Azabicyclo[2.2.2]oct-3-yl- 2,3-dihydro-1,4-benzodioxin-6-carboxamide fumarate
Application:
PHA 568487 is an agonist of AChR α7
CAS Number:
527680-56-4
Molecular Weight:
404.41
Molecular Formula:
C16H20N2O3•C4H4O4
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
Available in US only.
Available in US only.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
PHA 568487 is a selective and potent inhibitor of cyclin-dependent kinase 9 (CDK9). It functions by binding to the ATP-binding site of CDK9, thereby preventing the phosphorylation of RNA polymerase II and inhibiting transcription. Pha 568487′s mechanism of action disrupts the cell cycle and leads to the accumulation of cells in the G1 phase, ultimately inducing apoptosis in cancer cells. PHA 568487 may downregulate the expression of anti-apoptotic proteins, further contributing to its pro-apoptotic effects. Its ability to target CDK9 may be a useful for studying the regulation of transcription.
PHA 568487 (CAS 527680-56-4) References
- Multiple species metabolism of PHA-568487, a selective alpha 7 nicotinic acetylcholine receptor agonist. | Shilliday, FB., et al. 2010. Drug Metab Lett. 4: 162-72. PMID: 20642449
- Resolving postoperative neuroinflammation and cognitive decline. | Terrando, N., et al. 2011. Ann Neurol. 70: 986-995. PMID: 22190370
- Dysfunction of inflammation-resolving pathways is associated with exaggerated postoperative cognitive decline in a rat model of the metabolic syndrome. | Su, X., et al. 2013. Mol Med. 18: 1481-90. PMID: 23296426
- Contribution of α7 nicotinic receptor to airway epithelium dysfunction under nicotine exposure. | Maouche, K., et al. 2013. Proc Natl Acad Sci U S A. 110: 4099-104. PMID: 23431157
- Donepezil and the alpha-7 agonist PHA 568487, but not risperidone, ameliorate spatial memory deficits in a subchronic MK-801 mouse model of cognitive impairment in schizophrenia. | Karamihalev, S., et al. 2014. Behav Brain Res. 272: 248-51. PMID: 25036424
- Alpha-7 nicotinic acetylcholine receptor agonist treatment reduces neuroinflammation, oxidative stress, and brain injury in mice with ischemic stroke and bone fracture. | Han, Z., et al. 2014. J Neurochem. 131: 498-508. PMID: 25040630
- Stimulation of the α7 nicotinic acetylcholine receptor protects against neuroinflammation after tibia fracture and endotoxemia in mice. | Terrando, N., et al. 2015. Mol Med. 20: 667-75. PMID: 25365546
- Reducing inflammation and rescuing FTD-related behavioral deficits in progranulin-deficient mice with α7 nicotinic acetylcholine receptor agonists. | Minami, SS., et al. 2015. Biochem Pharmacol. 97: 454-462. PMID: 26206194
- Activation of Alpha-7 Nicotinic Acetylcholine Receptor Reduces Brain Edema in Mice with Ischemic Stroke and Bone Fracture. | Zou, D., et al. 2017. Mol Neurobiol. 54: 8278-8286. PMID: 27914011
- Inflammation in stroke: the role of cholinergic, purinergic and glutamatergic signaling. | Martín, A., et al. 2018. Ther Adv Neurol Disord. 11: 1756286418774267. PMID: 29774059
- Reduction of neuroinflammation alleviated mouse post bone fracture and stroke memory dysfunction. | Huo, K., et al. 2021. J Cereb Blood Flow Metab. 41: 2162-2173. PMID: 33641516
Activator of:
AChR α 7.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
PHA 568487, 10 mg | sc-204186 | 10 mg | $101.00 | |||
| US: Only available in the US | ||||||
PHA 568487, 50 mg | sc-204186A | 50 mg | $575.00 | |||
| US: Only available in the US | ||||||