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AC260584

Catalog No.GC30859

AC260584 is an M1 muscarinic receptor allosteric agonist with a pEC50 of 7.6.

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AC260584 Chemical Structure

Cas No.: 560083-42-3

Size Price Stock Qty
10mM (in 1mL DMSO)
$233.00
In stock
1mg
$101.00
In stock
5mg
$304.00
In stock
10mg
$459.00
In stock
50mg
$1,379.00
In stock
100mg
$1,930.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Animal experiment:

Rats: AC260584 is formulated in 100% 50 mM sodium acetate buffer pH 4.5 at a concentration of 1 mg/mL. Dosing solution is at room temperature prior to dosing. Three rats are administered AC260584 (2 mg/kg) intravenously and three rats are administered the drug orally (10 mg/kg). Rats dosed intravenously are catheterized at the jugular and femoral vein, while those dosed orally are catheterized only at the femoral vein. Rats are housed individually, fasted overnight and dosed by individual body weight. Plasma samples are collected at several time points and analyzed by LC/MS/MS[1].

References:

[1]. Bradley SR, et al. AC260584, an orally bioavailable M(1) muscarinic receptor allosteric agonist, improves cognitive performance in an animal model. Neuropharmacology. 2010 Feb;58(2):365-73.
[2]. Li Z, et al. AC260584 (4-[3-(4-butylpiperidin-1-yl)-propyl]-7-fluoro-4H-benzo[1,4]oxazin-3-one), a selective muscarinic M1 receptor agonist, increases acetylcholine and dopamine release in rat medial prefrontal cortex and hippocampus. Eur J Pharmacol. 2007 Oct 31;572(2-3):129-37.

Background

AC260584 is an M1 muscarinic receptor allosteric agonist with a pEC50 of 7.6.

AC260584 is found to be a potent (pEC50=7.6-7.7) and efficacious (90-98% of carbachol) muscarinic M1 receptor agonist. AC260584 shows functional selectivity for the M1 receptor over the M2, M3, M4 and M5 muscarinic receptor subtypes. Its selectivity is found to be similar in native tissues expressing mAChRs to its profile in recombinant systems[1].

In rodents, AC260584 activates extracellular signal regulated kinase 1 and 2 (ERK1/2) phosphorylation in the hippocampus, prefrontal cortex and perirhinal cortex. The ERK1/2 activation is dependent upon muscarinic M1 receptor activation since it is not observed in M1 knockout mice. AC260584 also improves the cognitive performance of mice in the novel object recognition assay and its action is blocked by the muscarinic receptor antagonist pirenzepine. In addition, AC260584 is found to be orally bioavailable in rodents[1]. AC260584 at 3 and 10 mg/kg significantly increases dopamine release in the medial prefrontal cortex and hippocampus. However, only the high dose of AC260584, 10 mg/kg (s.c.), significantly increases acetylcholine release in these regions[2].

[1]. Bradley SR, et al. AC260584, an orally bioavailable M(1) muscarinic receptor allosteric agonist, improves cognitive performance in an animal model. Neuropharmacology. 2010 Feb;58(2):365-73. [2]. Li Z, et al. AC260584 (4-[3-(4-butylpiperidin-1-yl)-propyl]-7-fluoro-4H-benzo[1,4]oxazin-3-one), a selective muscarinic M1 receptor agonist, increases acetylcholine and dopamine release in rat medial prefrontal cortex and hippocampus. Eur J Pharmacol. 2007 Oct 31;572(2-3):129-37.

Chemical Properties

Cas No. 560083-42-3 SDF
Canonical SMILES O=C1COC2=CC(F)=CC=C2N1CCCN3CCC(CCCC)CC3
Formula C20H29FN2O2 M.Wt 348.45
Solubility DMSO : ≥ 50 mg/mL (143.49 mM);Water : < 0.1 mg/mL (insoluble) 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 2.8699 mL 14.3493 mL 28.6985 mL
5 mM 0.574 mL 2.8699 mL 5.7397 mL
10 mM 0.287 mL 1.4349 mL 2.8699 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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Average Rating: 5 ★★★★★ (Based on Reviews and 20 reference(s) in Google Scholar.)

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