1. GPCR/G Protein Neuronal Signaling
  2. mAChR
  3. AC260584

AC260584 is an M1 muscarinic receptor allosteric agonist with a pEC50 of 7.6.

For research use only. We do not sell to patients.

AC260584 Chemical Structure

AC260584 Chemical Structure

CAS No. : 560083-42-3

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

1 Publications Citing Use of MCE AC260584

View All mAChR Isoform Specific Products:

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

AC260584 is an M1 muscarinic receptor allosteric agonist with a pEC50 of 7.6.

IC50 & Target

mAChR1

 

In Vitro

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.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

348.45

Formula

C20H29FN2O2

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1COC2=CC(F)=CC=C2N1CCCN3CCC(CCCC)CC3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

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.

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (7.17 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation
References
Animal Administration
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

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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AC260584 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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AC260584
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