| Size | Price | Stock | Qty |
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| 1mg |
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| Targets |
The primary target of AC-260584 is the muscarinic M1 receptor, a G protein-coupled receptor that plays a key role in cognitive function and neural plasticity. It acts as an allosteric agonist, binding to a site distinct from the orthosteric binding site and modulating receptor activity. By activating M1 receptors, AC-260584 enhances cholinergic signaling, which is involved in learning, memory, and attention.
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| ln Vitro |
The results showed that AC260584 is a strong muscarinic M1 receptor agonist (pEC50=7.6-7.7) and potent (90-98% of carbachol). Functional selectivity for the M1 receptor over the M2, M3, M4, and M5 muscarinic receptor subtypes is demonstrated by AC260584. Its spectrum in recombinant systems was shown to be similar to its selectivity in natural tissues expressing mAChR [1].
In vitro, AC-260584 is a potent muscarinic M1 receptor agonist with a pEC₅₀ of 7.6-7.7. It exhibits strong agonism, with 90-98% of the efficacy of carbachol, a full agonist. Its activity is characterized in cell-based assays measuring receptor activation and downstream signaling, such as calcium mobilization or inositol phosphate accumulation. |
| ln Vivo |
In rodents, the hippocampus, prefrontal cortex, and perirhinal cortex exhibit phosphorylation of extracellular signal-regulated kinase 1 and 2 (ERK1/2) upon activation by AC260584. Since M1 mutant animals did not exhibit this activation, ERK1/2 activation was reliant on muscarinic M1 receptor activation. In a unique object recognition test, AC260584 also enhanced mice's cognitive function; pirenzepine, a muscarinic receptor antagonist, prevented this benefit. Furthermore, it was discovered that AC260584 is orally accessible in rodents [1]. Dopamine release was markedly enhanced in the medial prefrontal cortex and hippocampus by AC260584 at doses of 3 and 10 mg/kg. However, the release of acetylcholine in these locations was only markedly augmented by a high dose of AC260584 (10 mg/kg (sc)) [2].
In vivo, AC-260584 has a behavioral profile consistent with antipsychotic-like efficacy with the potential to improve cognitive performance. It shows reduced liability for extrapyramidal symptoms, which are common side effects of many antipsychotic drugs. The compound is orally bioavailable, making it suitable for in vivo administration. Its effects on cognitive function and behavior have been studied in animal models. |
| Enzyme Assay |
In vitro receptor binding studies for AC-260584 measure its affinity for the muscarinic M1 receptor. Radioligand competition assays are performed using membrane preparations from cells expressing the M1 receptor. The compound competes with a labeled ligand, and the affinity is determined. Selectivity over other muscarinic receptor subtypes (M2-M5) is assessed to confirm its specificity.
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| Cell Assay |
In vitro cell-based functional assays for AC-260584 evaluate its agonist activity at the M1 receptor. Cells expressing the M1 receptor are treated with the compound, and receptor activation is measured by downstream signaling, such as calcium mobilization or inositol phosphate accumulation. The compound's potency (pEC₅₀) and efficacy are determined from dose-response curves.
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| Animal Protocol |
In vivo animal studies for AC-260584 are conducted in models of cognitive dysfunction and psychiatric disorders. The compound is administered orally, and its effects on cognitive performance, such as memory and attention, are assessed using behavioral tests. Its antipsychotic-like efficacy is evaluated in models of psychosis. Pharmacokinetic studies determine the compound's half-life and bioavailability.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of AC-260584 are consistent with an orally bioavailable compound. Its molecular weight is 348.45 g/mol. For research use, it is typically stored as a powder at -20°C. Further details on its half-life, Cmax, and bioavailability are available from the primary research literature.
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| Toxicity/Toxicokinetics |
The toxicity profile of AC-260584 has been evaluated in preclinical studies. It shows reduced liability for extrapyramidal symptoms, which are common side effects of many antipsychotic drugs. As a muscarinic agonist, its potential side effects may include cholinergic effects such as nausea, diarrhea, and sweating. The compound is for research use only and is not intended for human therapeutic applications.
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| References |
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| Additional Infomation |
Additional information: AC-260584 is also known as AC260584. It is a selective M1 muscarinic receptor allosteric agonist with a pEC₅₀ of 7.6. The compound has a behavioral profile consistent with antipsychotic-like efficacy and cognitive enhancement. This product is for research use only and is not approved for clinical or therapeutic applications.
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| Molecular Formula |
C20H29FN2O2
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|---|---|
| Molecular Weight |
348.454869031906
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| Exact Mass |
348.221
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| CAS # |
560083-42-3
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| PubChem CID |
9928284
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| Appearance |
White to off-white solid powder
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| LogP |
3.846
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
25
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| Complexity |
426
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
BWAKMLKESHKOHK-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H29FN2O2/c1-2-3-5-16-8-12-22(13-9-16)10-4-11-23-18-7-6-17(21)14-19(18)25-15-20(23)24/h6-7,14,16H,2-5,8-13,15H2,1H3
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| Chemical Name |
4-[3-(4-butylpiperidin-1-yl)propyl]-7-fluoro-1,4-benzoxazin-3-one
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 50 mg/mL (~143.49 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.17 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.17 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8699 mL | 14.3493 mL | 28.6985 mL | |
| 5 mM | 0.5740 mL | 2.8699 mL | 5.7397 mL | |
| 10 mM | 0.2870 mL | 1.4349 mL | 2.8699 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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