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

AC260584 

Cat. No.: HY-100336 Purity: 99.25%
Handling Instructions

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

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 304 In-stock
Estimated Time of Arrival: December 31
1 mg USD 132 In-stock
Estimated Time of Arrival: December 31
5 mg USD 396 In-stock
Estimated Time of Arrival: December 31
10 mg USD 600 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1800 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2520 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

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

IC50 & Target

pEC50: 7.6 (M1)[1]

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].

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].

Molecular Weight

348.45

Formula

C₂₀H₂₉FN₂O₂

CAS No.

560083-42-3

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 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 50 mg/mL (143.49 mM)

H2O : < 0.1 mg/mL (insoluble)

*"≥" 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
10 mM 0.2870 mL 1.4349 mL 2.8699 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
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
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Keywords:

AC260584AC 260584AC-260584mAChRMuscarinic acetylcholine receptorInhibitorinhibitorinhibit

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AC260584
Cat. No.:
HY-100336
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