AC260584 |
Catalog No.GC30859 |
AC260584 is an M1 muscarinic receptor allosteric agonist with a pEC50 of 7.6.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 560083-42-3
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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. |
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.
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. |
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Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
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. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
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