| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
M2 muscarinic acetylcholine receptor (mAChR). Arecaidine but-2-ynyl ester tosylate (ABET) is a selective agonist at this receptor.
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|---|---|
| ln Vitro |
Arecaidine but-2-ynyl ester tosylate (ABET) is a selective mAChR M2 agonist. As an M2 agonist, it activates M2 receptors, which are coupled to Gi/o proteins and mediate inhibitory responses such as bradycardia and reduced contractility in the heart. The compound dose-dependently decreases mean arterial pressure and heart rate in rats.
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| ln Vivo |
In vivo, ABET dose-dependently decreases mean arterial pressure and heart rate in rats. This effect is consistent with the role of M2 receptors in mediating bradycardia and vasodilation. The compound has been studied for its potential applications in cardiovascular disease research.
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| Enzyme Assay |
In vitro receptor binding assays for ABET are performed to evaluate its affinity for the M2 receptor and its selectivity over other mAChR subtypes. Radioligand binding studies using membrane preparations from cells expressing M1-M5 receptors are conducted. The compound's ability to displace a specific radiolabeled ligand from each receptor subtype is measured to calculate its binding affinities.
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| Cell Assay |
In vitro cell-based assays are conducted using cells expressing recombinant M2 receptors. The cells are treated with ABET, and receptor activation is measured by assessing downstream signaling events such as inhibition of cAMP accumulation or activation of G protein-coupled inwardly rectifying potassium channels (GIRKs). The potency and efficacy of the compound at M2 are determined from these functional assays.
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| Animal Protocol |
In vivo studies are conducted in animal models to evaluate the cardiovascular effects of ABET. The compound is administered via various routes, and its effects on heart rate, blood pressure, and cardiac function are assessed. The dose-dependent decrease in mean arterial pressure and heart rate in rats has been demonstrated.
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| ADME/Pharmacokinetics |
No detailed pharmacokinetic data are publicly available for ABET. As a research compound, its ADME properties would be characterized in standard preclinical studies to guide in vivo experiments. The compound's oral bioavailability and duration of action are key parameters for its use in cardiovascular research.
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| Toxicity/Toxicokinetics |
No specific toxicity data are publicly available for ABET. As an M2 receptor agonist, its toxicity profile would be expected to be related to its mechanism of action. Excessive M2 receptor activation can lead to severe bradycardia, hypotension, and cardiac arrest.
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| References |
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| Additional Infomation |
Arecaidine but-2-ynyl ester tosylate (ABET) is a selective M2 muscarinic receptor agonist that dose-dependently decreases mean arterial pressure and heart rate in rats. It is used as a research tool to study the role of M2 receptors in cardiovascular function and disease. The compound is not approved for human therapeutic use and is strictly for research purposes. It has the CAS number 119630-77-2.
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| Molecular Formula |
C18H23NO5S
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|---|---|
| Molecular Weight |
365.44
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| Exact Mass |
365.129
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| CAS # |
119630-77-2
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| PubChem CID |
6604935
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
25
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| Complexity |
512
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC#CCOC(=O)C1=CCCN(C1)C.CC1=CC=C(C=C1)S(=O)(=O)O
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| InChi Key |
GKPXMGUNTQSFGA-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C11H15NO2.C7H8O3S/c1-3-4-8-14-11(13)10-6-5-7-12(2)9-10;1-6-2-4-7(5-3-6)11(8,9)10/h6H,5,7-9H2,1-2H3;2-5H,1H3,(H,8,9,10)
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| Chemical Name |
but-2-ynyl 1-methyl-3,6-dihydro-2H-pyridine-5-carboxylate;4-methylbenzenesulfonic acid
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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: 125 mg/mL (342.05 mM)
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7364 mL | 13.6821 mL | 27.3643 mL | |
| 5 mM | 0.5473 mL | 2.7364 mL | 5.4729 mL | |
| 10 mM | 0.2736 mL | 1.3682 mL | 2.7364 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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