AC260584
Based on 1 publication(s) in Google Scholar
AC260584 is an M1 muscarinic receptor allosteric agonist with a pEC50 of 7.6.
For research use only. We do not sell to patients.
- Purity: 99.48%
- CAS No.: 560083-42-3
- Formula: C20H29FN2O2
- Molecular Weight:348.45
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) AC260584
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Biological Activity
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mAChR1 |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 560083-42-3
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Appearance Solid
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Molecular Weight 348.45
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Formula C20H29FN2O2
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Color White to off-white
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SMILES
O=C1COC2=CC(F)=CC=C2N1CCCN3CCC(CCCC)CC3
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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ACS Chem Neurosci
Discovery of Procognitive Antipsychotics by Combining Muscarinic M1 Receptor Structure-Activity Relationship with Systems Response Profiles in Zebrafish Larvae. [Abstract]2020 Jan 15;11(2):173-183. PMID: 31850734
Solvent & Solubility
DMSO : ≥ 50 mg/mL (143.49 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.17 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (274 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.8699 mL | 14.3493 mL | 28.6985 mL | 71.7463 mL |
| 5 mM | 0.5740 mL | 2.8699 mL | 5.7397 mL | 14.3493 mL | |
| 10 mM | 0.2870 mL | 1.4349 mL | 2.8699 mL | 7.1746 mL | |
| 15 mM | 0.1913 mL | 0.9566 mL | 1.9132 mL | 4.7831 mL | |
| 20 mM | 0.1435 mL | 0.7175 mL | 1.4349 mL | 3.5873 mL | |
| 25 mM | 0.1148 mL | 0.5740 mL | 1.1479 mL | 2.8699 mL | |
| 30 mM | 0.0957 mL | 0.4783 mL | 0.9566 mL | 2.3915 mL | |
| 40 mM | 0.0717 mL | 0.3587 mL | 0.7175 mL | 1.7937 mL | |
| 50 mM | 0.0574 mL | 0.2870 mL | 0.5740 mL | 1.4349 mL | |
| 60 mM | 0.0478 mL | 0.2392 mL | 0.4783 mL | 1.1958 mL | |
| 80 mM | 0.0359 mL | 0.1794 mL | 0.3587 mL | 0.8968 mL | |
| 100 mM | 0.0287 mL | 0.1435 mL | 0.2870 mL | 0.7175 mL |
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