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A 844606

Catalog No.GC15333

α7 nAChR partial agonist

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A 844606 Chemical Structure

Cas No.: 861119-08-6

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10mg
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

A 844606 is a potent and selective partial agonist of α7 nicotinic acetylcholine receptor (nAChR) with IC50 value of 11 nM [1].

The α7 nAChR is a nicotinic acetylcholine receptor and is located in the brain, spleen and lymphocytes of lymph nodes. The α7 nAChR plays an important role in the pathophysiology of neuropsychiatric diseases such as Alzheimer’s disease, schizophrenia, drug addiction and depression [2].

A 844606 is a potent and selective α7 nAChR partial agonist with IC50 values of 11 and >30000 nM for α7 and α4β2, respectively. In Xenopus oocytes expressed recombinant human and rat α7 nAChR, A 844606 showed agonist activity with EC50 values of 1.4 and 2.2 μM, respectively. In PC12 cells, A 844606 activated α7 nAChR, which stimulated ERK1/2 phosphorylation [1].

In the mouse brain, A 844606 showed high uptake. In monkey brain, A 844606 was mainly distributed in the thalamus and hippocampus and was low in the cerebellum. Also, A 844606 was reduced by pretreatment with SSR180711, an α7 nAChR agonist [2].

References:
[1].  Briggs CA, Schrimpf MR, Anderson DJ, et al. alpha7 nicotinic acetylcholine receptor agonist properties of tilorone and related tricyclic analogues. Br J Pharmacol, 2008, 153(5): 1054-1061.
[2].  Toyohara J, Ishiwata K, Sakata M, et al. In vivo evaluation of alpha7 nicotinic acetylcholine receptor agonists [11C]A-582941 and [11C]A-844606 in mice and conscious monkeys. PLoS One, 2010, 5(2): e8961.

Chemical Properties

Cas No. 861119-08-6 SDF
Chemical Name 2-((3aR,6aR)-5-methylhexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl)-9H-xanthen-9-one
Canonical SMILES O=C1C2=CC(N3C[C@@H](CN(C)C4)[C@H]4C3)=CC=C2OC5=CC=CC=C15
Formula C20H20N2O2 M.Wt 320.38
Solubility <1.6mg/ml in ethanol Storage Store at -20°C
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.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 3.1213 mL 15.6065 mL 31.2129 mL
5 mM 0.6243 mL 3.1213 mL 6.2426 mL
10 mM 0.3121 mL 1.5606 mL 3.1213 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 19 reference(s) in Google Scholar.)

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