AR-R 17779 hydrochloride |
| Catalog No.GC11060 |
Le chlorhydrate d'AR-R 17779 est un agoniste complet puissant et sélectif du nAChR, avec un Kis de 92 et 16 000 nM pour les sous-types α7 et α4β2, respectivement.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 178419-42-6
Sample solution is provided at 25 µL, 10mM.
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AR-R 17779 is a selective agonist of α7 nicotinic acetylcholine receptor (α7-nAChR) [1] with an EC50 of 21 μM to rat α7-nAChRs expressed in Xenopus oocytes [2].
Nicotine enhances cognitive functions, e.g. learning, attention, retention and memory in both humans and animals, via activation of brain nicotinic acetylcholine receptors (nAChRs). These receptors are homo- or heteropentameric ligand-gated ion channels. The most common nicotinic receptors found in the brain are the α4β2-nAChR and the α7-nAChR [3].
The expression of CD38, CD138, and Bcl-6, was sensitive to regulation via nAChRs. Daudi cells exposed to AR-R 17779 ± methyllycaconitine (MLA) resulted in only moderate changes in the gene expression of CD38, CD138 and Bcl-6, but AR-R 17779 alone significantly (P< 0.05) increased protein levels of CD38 and CD138. That means the effect of AR-R 17779 was abolished by MLA [4].
Cholesterol is necessary for the homeostasis of acetylcholine receptor (AChR) levels for ion translocation and at the plasmalemma [5]. In ApoE-deficient mice, AR-R 17779 significantly reduced atherosclerotic plaque area in the thoracic aorta, and lowered heart rate, blood pressure, serum triglyceride level and serum total cholesterol level compared with which in Ang II + HFD mice. Treatment with AR-R 17779 in mice did not result in any sickness behavior or apparent abnormalities. At the end of the experiment, the serum concentration of AR-R 17779 was 1.18 ± 0.17 μM. In ApoE-deficient mice, treatment with AR-R 17779 resulted in significantly reduced aortic diameter comparable to control mice (0.81 ± 0.11 mm, p< 0.0001 vs. Ang II + HFD) [1].
References:
[1]. Toru Hashimoto, Toshihiro Ichiki, AyaWatanabe, et al. Stimulation of α7 nicotinic acetylcholine receptor by AR-R17779 suppresses atherosclerosis and aortic aneurysm formation in apolipoprotein E-deficient mice. Vascular Pharmacology, 2014, 61:49-55.
[2]. Rudy Schreiber, Marion Dalmus and Jean De Vry. Effects of α4/β2- and α7-nicotine acetylcholine receptor agonists on prepulse inhibition of the acoustic startle response in rats and mice. Psychopharmacology, 2002, 159:248-257.
[3]. Marja van Kampen, Karin Selbach, Renate Schneider, et al. AR-R 17779 improves social recognition in rats by activation of nicotinic α7 receptors. Psychopharmacology, 2004, 172:375-383.
[4]. Juan Arredondo, Denys Omelchenko, Alexander I Chernyavsky, et al. Functional role of the nicotinic arm of the acetylcholine regulatory axis in human B-cell lines. Journal of Experimental Pharmacology, 2009, 1:1-7.
[5]. Virginia Borroni and Francisco J. Barrantes. Cholesterol Modulates the Rate and Mechanism of Acetylcholine Receptor Internalization. J. Biol. Chem., 2011, 286(19):17122-32.
| Cas No. | 178419-42-6 | SDF | |
| Chemical Name | (1'R,3'S,4'R)-1'-azaspiro[oxazolidine-5,3'-bicyclo[2.2.2]octan]-2-one hydrochloride | ||
| Canonical SMILES | O=C(NC1)O[C@]21[C@H](CC3)CC[N@]3C2.Cl | ||
| Formula | C9H14N2O2.HCl | M.Wt | 218.68 |
| Solubility | <10.93mg/ml in DMSO; <21.87mg/ml in Water | Storage | Desiccate at RT |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 4.5729 mL | 22.8645 mL | 45.7289 mL |
| 5 mM | 0.9146 mL | 4.5729 mL | 9.1458 mL |
| 10 mM | 0.4573 mL | 2.2864 mL | 4.5729 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 28 reference(s) in Google Scholar.)
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