PHA 543613 hydrochlorideCAS# 478149-53-0 |
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Quality Control & MSDS
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| Cas No. | 478149-53-0 | SDF | Download SDF |
| PubChem ID | 56972222 | Appearance | Powder |
| Formula | C15H18ClN3O2 | M.Wt | 307.78 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble to 100 mM in water and to 25 mM in DMSO | ||
| Chemical Name | N-[(3R)-1-azabicyclo[2.2.2]octan-3-yl]furo[2,3-c]pyridine-5-carboxamide;hydrochloride | ||
| SMILES | C1CN2CCC1C(C2)NC(=O)C3=NC=C4C(=C3)C=CO4.Cl | ||
| Standard InChIKey | YMTPSZUBRSEWNY-ZOWNYOTGSA-N | ||
| Standard InChI | InChI=1S/C15H17N3O2.ClH/c19-15(12-7-11-3-6-20-14(11)8-16-12)17-13-9-18-4-1-10(13)2-5-18;/h3,6-8,10,13H,1-2,4-5,9H2,(H,17,19);1H/t13-;/m0./s1 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Potent α7 nAChR agonist that displays selectivity over α3β4, α1β1γδ, α4β2 and 5-HT3 receptors. Positively influences sensory gating and memory in in vivo models of schizophrenia. Orally active and brain penetrant. |
PHA 543613 hydrochloride Dilution Calculator
PHA 543613 hydrochloride Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 3.2491 mL | 16.2454 mL | 32.4907 mL | 64.9815 mL | 81.2269 mL |
| 5 mM | 0.6498 mL | 3.2491 mL | 6.4981 mL | 12.9963 mL | 16.2454 mL |
| 10 mM | 0.3249 mL | 1.6245 mL | 3.2491 mL | 6.4981 mL | 8.1227 mL |
| 50 mM | 0.065 mL | 0.3249 mL | 0.6498 mL | 1.2996 mL | 1.6245 mL |
| 100 mM | 0.0325 mL | 0.1625 mL | 0.3249 mL | 0.6498 mL | 0.8123 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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The alpha 7 nicotinic receptor agonist PHA-543613 hydrochloride inhibits Porphyromonas gingivalis-induced expression of interleukin-8 by oral keratinocytes.[Pubmed:24609617]
Inflamm Res. 2014 Jul;63(7):557-68.
OBJECTIVE: The alpha 7 nicotinic receptor (alpha7nAChR) is expressed by oral keratinocytes. alpha7nAChR activation mediates anti-inflammatory responses. The objective of this study was to determine if alpha7nAChR activation inhibited pathogen-induced interleukin-8 (IL-8) expression by oral keratinocytes. MATERIALS AND METHODS: Periodontal tissue expression of alpha7nAChR was determined by real-time PCR. OKF6/TERT-2 oral keratinocytes were exposed to Porphyromonas gingivalis in the presence and absence of a alpha7nAChR agonist (PHA-543613 hydrochloride) alone or after pre-exposure to a specific alpha7nAChR antagonist (alpha-bungarotoxin). Interleukin-8 (IL-8) expression was measured by ELISA and real-time PCR. Phosphorylation of the NF-kappaB p65 subunit was determined using an NF-kappaB p65 profiler assay and STAT-3 activation by STAT-3 in-cell ELISA. The release of ACh from oral keratinocytes in response to P. gingivalis lipopolysaccharide was determined using a GeneBLAzer M3 CHO-K1-bla cell reporter assay. RESULTS: Expression of alpha7nAChR mRNA was elevated in diseased periodontal tissue. PHA-543613 hydrochloride inhibited P. gingivalis-induced expression of IL-8 at the transcriptional level. This effect was abolished when cells were pre-exposed to a specific alpha7nAChR antagonist, alpha-bungarotoxin. PHA-543613 hydrochloride downregulated NF-kappaB signalling through reduced phosphorylation of the NF-kappaB p65-subunit. In addition, PHA-543613 hydrochloride promoted STAT-3 signalling by maintenance of phosphorylation. Furthermore, oral keratinocytes upregulated ACh release in response to P. gingivalis lipopolysaccharide. CONCLUSION: These data suggest that alpha7nAChR plays a role in regulating the innate immune responses of oral keratinocytes.
Discovery of N-[(3R)-1-azabicyclo[2.2.2]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide, an agonist of the alpha7 nicotinic acetylcholine receptor, for the potential treatment of cognitive deficits in schizophrenia: synthesis and structure--activity relationship.[Pubmed:16821801]
J Med Chem. 2006 Jul 13;49(14):4425-36.
N-[(3R)-1-Azabicyclo[2.2.2]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide (14, PHA-543,613), a novel agonist of the alpha7 neuronal nicotinic acetylcholine receptor (alpha7 nAChR), has been identified as a potential treatment of cognitive deficits in schizophrenia. Compound 14 is a potent and selective alpha7 nAChR agonist with an excellent in vitro profile. The compound is characterized by rapid brain penetration and high oral bioavailability in rat and demonstrates in vivo efficacy in auditory sensory gating and, in an in vivo model to assess cognitive performance, novel object recognition.
