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AC260584

Catalog No. T14092   CAS 560083-42-3

AC260584 is an M1 muscarinic receptor allosteric agonist (pEC50: 7.6).

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AC260584 Chemical Structure
AC260584, CAS 560083-42-3
Pack Size Availability Price/USD Quantity
5 mg 6-8 weeks $ 327.00
25 mg 6-8 weeks $ 1,140.00
50 mg 6-8 weeks $ 1,490.00
100 mg 6-8 weeks $ 1,990.00
1 mL * 10 mM (in DMSO) 6-8 weeks $ 270.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description AC260584 is an M1 muscarinic receptor allosteric agonist (pEC50: 7.6).
Targets&IC50 M1:(pEC50)7.6
In vitro AC260584 is identified as a potent (pEC50=7.6-7.7) and efficacious (90-98% of carbachol) agonist for the muscarinic M1 receptor, exhibiting significant functional selectivity over the M2, M3, M4, and M5 subtypes of muscarinic receptors. This selectivity profile of AC260584 is consistent across native tissues expressing mAChRs and recombinant systems.
In vivo In rodent studies, AC260584 has been shown to activate the phosphorylation of extracellular signal-regulated kinase 1 and 2 (ERK1/2) in the hippocampus, prefrontal cortex, and perirhinal cortex. This activation is contingent upon the activation of muscarinic M1 receptors, as evidenced by its absence in M1 receptor knockout mice. Furthermore, AC260584 enhances cognitive performance in mice, as demonstrated in the novel object recognition test, with this effect being inhibited by the muscarinic receptor antagonist pirenzepine. Additionally, AC260584 has been noted for its oral bioavailability in rodents. At doses of 3 and 10 mg/kg, AC260584 significantly boosts dopamine release in the medial prefrontal cortex and hippocampus, while only the 10 mg/kg dose notably increases acetylcholine release in these areas.
Molecular Weight 348.45
Formula C20H29FN2O2
CAS No. 560083-42-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (143.49 mM)

TargetMolReferences and Literature

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.

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Keywords

AC260584 560083-42-3 Others AC 260584 AC-260584 inhibitor inhibit

 

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