| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
Muscarinic acetylcholine receptors (mAChRs), primarily M2 receptors. Oxotremorine sesquifumarate is an mAChR agonist.
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| ln Vitro |
In vitro, oxotremorine (10.5 μM) paralyzes the rat diaphragm's twitch responses to both direct and indirect stimulation[1].
Oxotremorine sesquifumarate is a muscarinic acetylcholine receptor agonist that primarily activates M2 receptors. 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. In the central nervous system, M2 receptors act as presynaptic autoreceptors that inhibit acetylcholine release. |
| ln Vivo |
Oxotremorine (10, 5, 2 1 μg; 10 μL) dose-dependently decreases tactile hypersensitivity in rats with sciatic nerve injuries[2].
In vivo, oxotremorine is known to produce a range of effects related to muscarinic receptor activation, including tremor, hypothermia, analgesia, and bradycardia. The compound is used in research to study the role of muscarinic receptors in various physiological and pathological processes. It has been used in neurological research. |
| Enzyme Assay |
In vitro receptor binding assays for oxotremorine are performed to evaluate its affinity for muscarinic receptor 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 muscarinic receptor subtypes. The cells are treated with oxotremorine, and receptor activation is measured by assessing downstream signaling events such as inhibition of cAMP accumulation (for M2/M4) or calcium mobilization (for M1/M3/M5). The potency and efficacy of the compound at each receptor subtype are determined from these functional assays.
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| Animal Protocol |
In vivo studies are conducted in animal models to evaluate the effects of oxotremorine on muscarinic receptor-mediated processes. The compound is administered via various routes, and its effects on tremor, body temperature, heart rate, and pain responses are assessed. The compound is used in neurological research.
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| ADME/Pharmacokinetics |
No detailed pharmacokinetic data are publicly available for oxotremorine sesquifumarate. As a research compound, its ADME properties would be characterized in standard preclinical studies to guide in vivo experiments.
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| Toxicity/Toxicokinetics |
No specific toxicity data are publicly available for oxotremorine sesquifumarate. As a muscarinic agonist, its toxicity profile would be expected to be related to its mechanism of action. Excessive muscarinic receptor activation can lead to cholinergic crisis, characterized by bradycardia, hypotension, salivation, lacrimation, urination, defecation, and muscle fasciculations.
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| References |
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| Additional Infomation |
Oxotremorine sesquifumarate is a muscarinic acetylcholine receptor agonist that primarily activates M2 receptors. It is used as a research tool to study muscarinic receptor function in the central and peripheral nervous systems. The compound is not approved for human therapeutic use and is strictly for research purposes. It has the CAS number 17360-35-9.
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| Molecular Formula |
C16H22N2O5
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|---|---|
| Molecular Weight |
380.40
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| Exact Mass |
760.317
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| CAS # |
17360-35-9
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| Related CAS # |
70-22-4;
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| PubChem CID |
6436473
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| Appearance |
White to off-white solid powder
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| Boiling Point |
373.9ºC at 760 mmHg
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| Melting Point |
102-105ºC(lit.)
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| Flash Point |
169.1ºC
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| Vapour Pressure |
8.7E-06mmHg at 25°C
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| LogP |
0.303
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
16
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
54
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| Complexity |
412
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1CN(CC1)CC#CCN2C(=O)CCC2.C1CN(CC1)CC#CCN2C(=O)CCC2.C(=C/C(=O)O)\C(=O)O.C(=C/C(=O)O)\C(=O)O.C(=C/C(=O)O)\C(=O)O
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| InChi Key |
WLYYOFJEBGHKEC-VQYXCCSOSA-N
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| InChi Code |
InChI=1S/2C12H18N2O.3C4H4O4/c2*15-12-6-5-11-14(12)10-4-3-9-13-7-1-2-8-13;3*5-3(6)1-2-4(7)8/h2*1-2,5-11H2;3*1-2H,(H,5,6)(H,7,8)/b;;3*2-1+
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| Chemical Name |
(E)-but-2-enedioic acid;1-(4-pyrrolidin-1-ylbut-2-ynyl)pyrrolidin-2-one
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| Synonyms |
oxotremorine sesquifumarate; DTXSID201017212; RefChem:169012; DTXCID001475400; 17360-35-9;
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 (328.60 mM)
H2O: 100 mg/mL (262.88 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.57 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.47 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.47 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6288 mL | 13.1441 mL | 26.2881 mL | |
| 5 mM | 0.5258 mL | 2.6288 mL | 5.2576 mL | |
| 10 mM | 0.2629 mL | 1.3144 mL | 2.6288 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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