Identification | Back Directory | [Name]
AC260584 | [CAS]
560083-42-3 | [Synonyms]
AC260584 AC-260584; AC 260584 2H-1,4-Benzoxazin-3(4H)-one, 4-[3-(4-butyl-1-piperidinyl)propyl]-7-fluoro- | [Molecular Formula]
C20H29FN2O2 | [MDL Number]
MFCD30533365 | [MOL File]
560083-42-3.mol | [Molecular Weight]
348.45 |
Chemical Properties | Back Directory | [Boiling point ]
525.6±50.0 °C(Predicted) | [density ]
1.098±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : ≥ 50 mg/mL (143.49 mM);Water : < 0.1 mg/mL (insoluble) | [form ]
Solid | [pka]
9.42±0.10(Predicted) | [color ]
White to off-white |
Hazard Information | Back Directory | [Uses]
AC260584 is an M1 muscarinic receptor allosteric agonist with a pEC50 of 7.6. | [in vivo]
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]. | [IC 50]
mAChR1 | [storage]
Store at -20°C | [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. DOI:10.1016/j.neuropharm.2009.10.003 [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. DOI:10.1016/j.ejphar.2007.06.025 |
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