| 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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| 250mg | |||
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| Targets |
5-HT3 antagonist 5 targets the serotonin 5-HT3 receptor, a ligand-gated ion channel. This receptor is predominantly found in the central and peripheral nervous systems and is involved in mediating the effects of serotonin, including nausea, vomiting, and pain. By acting as a 5-HT3 receptor antagonist, the compound blocks the binding of serotonin to the receptor, thereby inhibiting its signaling. This mechanism is useful in managing conditions like chemotherapy-induced nausea and vomiting (CINV) and irritable bowel syndrome (IBS). The compound has also shown antidepressant effects in mice.
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| ln Vitro |
In the longitudinal myenteric plexus preparation of guinea pig ileum, 5-HT3 antagonist 5 (compound 4c) demonstrated 5-HT3 receptor antagonism, specifically the 5-HT3 agonist 2-methyl-5-HT, with a pA2 value of 5[1].
In vitro, 5-HT3 antagonist 5 acts as a 5-HT3 receptor antagonist, exerting antagonism on 5-HT3 agonists and 2-methyl-5-HT. Its activity is demonstrated in receptor binding or functional assays where it inhibits the effects of 5-HT3 agonists. The compound's ability to block the 5-HT3 receptor makes it a valuable tool for studying the role of this receptor in various physiological and pathological processes. Its in vitro activity is characterized by its potency and selectivity for the 5-HT3 receptor. |
| ln Vivo |
Compound 4c, a 5-HT3 antagonist, has antidepressant properties and reduces the length of immobility in FST mice (1 mg/kg; i.p., single dose) [1].
In vivo, 5-HT3 antagonist 5 has demonstrated antidepressant effects in mice. In a forced swim test (FST), a single intraperitoneal dose of 1 mg/kg of the compound (referred to as compound 4c) reduced the length of immobility, indicating an antidepressant-like effect. This in vivo activity highlights its potential for treating depression and other neurological disorders. The compound's antidepressant effect is likely mediated through its antagonism of the 5-HT3 receptor, modulating serotonin signaling in the brain. |
| Enzyme Assay |
In vitro receptor binding assays for 5-HT3 antagonist 5 typically involve measuring its affinity for the 5-HT3 receptor. The compound is incubated with membrane preparations from cells expressing the 5-HT3 receptor and a radiolabeled ligand specific for the receptor. The amount of bound radioligand is measured in the presence of varying concentrations of the compound to determine its binding affinity (Ki). Functional assays, such as calcium flux assays, can also be used to measure the compound's ability to inhibit 5-HT3 receptor activation by agonists like 2-methyl-5-HT. The compound is typically dissolved in DMSO for stock solutions and diluted in the assay buffer.
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| Cell Assay |
In vitro cell-based assays for 5-HT3 antagonist 5 are performed in cell lines expressing the 5-HT3 receptor. Cells are loaded with a calcium-sensitive fluorescent dye and treated with varying concentrations of the compound. The cells are then stimulated with a 5-HT3 agonist (e.g., serotonin or 2-methyl-5-HT), and the increase in intracellular calcium is measured. The compound's ability to inhibit the agonist-induced calcium response is used to determine its antagonist activity. The compound is typically dissolved in DMSO and diluted in the cell culture medium for treatment.
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| Animal Protocol |
Animal/Disease Models: Swiss albino mice (23 ± 2 g) [1]
Doses: 1 mg/kg Route of Administration: intraperitoneal (ip) injection; single dose; test motor score results 10 minutes after Route of Administration: compared with vehicle treatment group (control group ), the duration of immobility is diminished compared to . No effect on locomotion in mice was observed during spontaneous locomotor activity. In vivo animal experiments with 5-HT3 antagonist 5 have been conducted in mice to evaluate its antidepressant effects. In a forced swim test (FST), mice were administered a single intraperitoneal dose of 1 mg/kg of the compound (compound 4c). The duration of immobility was then measured as an indicator of despair-like behavior. A reduction in immobility time compared to the control group indicated an antidepressant-like effect. This protocol demonstrates the compound's oral bioavailability and its potential for central nervous system activity. |
| ADME/Pharmacokinetics |
5-HT3 antagonist 5 has a molecular weight of 279.29 g/mol and the formula C16H13N3O2. It is also known as N-(4-methoxyphenyl)quinoxaline-2-carboxamide. The compound is intended for research use only and is not for human consumption. Its pharmacokinetic properties, such as absorption, distribution, metabolism, and excretion, have not been extensively characterized in the available literature. However, its antidepressant effect in mice after intraperitoneal administration suggests it can cross the blood-brain barrier.
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| Toxicity/Toxicokinetics |
Specific toxicological data for 5-HT3 antagonist 5 are not provided in the available sources. As a research chemical, its safety profile in humans has not been established. The compound is classified as a research reagent and is not for therapeutic or veterinary use. Standard laboratory safety precautions should be followed when handling this compound, including the use of appropriate personal protective equipment. Its purity is typically high (e.g., 99.75%).
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| References | |
| Additional Infomation |
5-HT3 antagonist 5 is a quinoxalin-2-carboxamide compound that acts as a 5-HT3 receptor antagonist. It has the molecular formula C16H13N3O2 and a molecular weight of 279.29 g/mol. The compound is also known as N-(4-methoxyphenyl)quinoxaline-2-carboxamide. As a 5-HT3 receptor antagonist, it blocks the effects of serotonin at the 5-HT3 receptor, which is involved in nausea and vomiting, as well as in gastrointestinal and neurological disorders. The compound has demonstrated antidepressant effects in mice, reducing immobility in the forced swim test at a dose of 1 mg/kg (i.p.). It is intended for research use only and is not for human consumption.
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| Molecular Formula |
C16H13N3O2
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| Molecular Weight |
279.293323278427
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| Exact Mass |
279.1
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| CAS # |
901599-43-7
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| PubChem CID |
4416580
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
2.9
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
21
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| Complexity |
355
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(C1C=NC2C(=CC=CC=2)N=1)NC1C=CC(OC)=CC=1
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| InChi Key |
UUFCEPQEIQOEAL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H13N3O2/c1-21-12-8-6-11(7-9-12)18-16(20)15-10-17-13-4-2-3-5-14(13)19-15/h2-10H,1H3,(H,18,20)
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| Chemical Name |
N-(4-methoxyphenyl)quinoxaline-2-carboxamide
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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 : ~20.83 mg/mL (~74.58 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 | 3.5805 mL | 17.9025 mL | 35.8051 mL | |
| 5 mM | 0.7161 mL | 3.5805 mL | 7.1610 mL | |
| 10 mM | 0.3581 mL | 1.7903 mL | 3.5805 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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