| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 100mg | |||
| Other Sizes |
| Targets |
FEMA-4809 targets the TRPM8 (transient receptor potential melastatin 8) receptor, a non-selective cation channel that is activated by cool temperatures (below 25°C) and by ligands such as (-)-menthol. As a potent TRPM8 receptor agonist, FEMA-4809 activates the channel and induces a cooling sensation. The compound has an EC50 of 0.2 nM for TRPM8 activation, making it one of the most potent TRPM8 agonists known.
|
|---|---|
| ln Vitro |
FEMA-4809 is a highly potent TRPM8 receptor agonist with an EC50 of 0.2 nM. Its activity can be assessed using cell-based assays in which cells expressing the human TRPM8 channel are treated with the compound and the resulting calcium influx is measured using a calcium-sensitive dye (e.g., Fluo-4). The EC50 for receptor activation is determined from dose-response curves. The compound's potency is significantly higher than that of (-)-menthol, making it a valuable tool for studying TRPM8 function.
|
| ln Vivo |
FEMA-4809 induces a cooling sensation through the activation of the TRPM8 ion channel. It is used as a cooling agent in the food and beverage industry for its distinct fruity and floral notes. The compound's high potency allows for its use at very low concentrations, minimizing any off-taste or other sensory effects. FEMA-4809 is a flavoring compound used to impart a cooling sensation to food and beverage products.
|
| Enzyme Assay |
Non-cellular assays for FEMA-4809 are limited as it is a receptor agonist that requires cellular context for activity. Its binding affinity for the TRPM8 receptor can be assessed using radioligand binding displacement studies with membrane preparations from cells expressing TRPM8. The membranes are incubated with a radiolabeled TRPM8 ligand and varying concentrations of FEMA-4809, and the IC50 is determined from displacement curves. The compound's physicochemical properties can be characterized using standard analytical techniques.
|
| Cell Assay |
In vitro cellular assays for FEMA-4809 involve treating cells expressing the human TRPM8 channel with the compound and measuring receptor-mediated calcium influx. Cells are loaded with a calcium-sensitive dye (e.g., Fluo-4) and treated with varying concentrations of FEMA-4809. The increase in intracellular calcium concentration is measured using a fluorescence plate reader. The EC50 for receptor activation is determined from dose-response curves. The compound's activity is compared to that of (-)-menthol and other TRPM8 agonists.
|
| Animal Protocol |
In vivo animal experiments are not applicable for FEMA-4809 as it is a flavoring compound and cooling agent used in food products, not a therapeutic agent. Its safety and efficacy are evaluated through sensory evaluation tests in humans and through toxicological studies. The compound is not administered to animals for pharmacological studies.
|
| ADME/Pharmacokinetics |
FEMA-4809 has a molecular weight of 327.40 and a molecular formula of C17H17N3O2S. It is a solid at room temperature and is typically stored at -20°C. Purity is ≥95%. The compound is soluble in DMSO (250 mg/mL, ultrasonic). It is stable under recommended storage conditions and is protected from light and moisture.
|
| Toxicity/Toxicokinetics |
FEMA-4809 is generally recognized as safe for use as a flavoring agent at the levels typically employed. Standard food safety precautions should be followed when handling the compound. As a TRPM8 agonist, it may cause a cooling sensation upon contact with skin or mucous membranes. Appropriate personal protective equipment should be used when handling the compound.
|
| References | |
| Additional Infomation |
FEMA-4809 (CAS 1374760-95-8) is a highly potent TRPM8 receptor agonist with an EC50 of 0.2 nM. It is a fully synthetic, non-naturally occurring phenoxyacetyl amide used as a cooling agent in the food and beverage industry. The compound activates the TRPM8 ion channel, which is responsible for cool perception. FEMA-4809 is available from various commercial suppliers for research and industrial applications.
|
| Molecular Formula |
C17H17N3O2S
|
|---|---|
| Molecular Weight |
327.400782346725
|
| Exact Mass |
327.104
|
| Elemental Analysis |
C, 62.37; H, 5.23; N, 12.83; O, 9.77; S, 9.79
|
| CAS # |
1374760-95-8
|
| PubChem CID |
67516108
|
| Appearance |
Off-white to light yellow solid powder
|
| LogP |
3.2
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
6
|
| Heavy Atom Count |
23
|
| Complexity |
388
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
QGDQESUNCJQMSA-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C17H17N3O2S/c1-13-4-6-14(7-5-13)22-12-17(21)20(16-8-9-18-19-16)11-15-3-2-10-23-15/h2-10H,11-12H2,1H3,(H,18,19)
|
| Chemical Name |
2-(4-methylphenoxy)-N-(1H-pyrazol-5-yl)-N-(thiophen-2-ylmethyl)acetamide
|
| Synonyms |
FEMA4809; FEMA 4809; FEMA-4809
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ~250 mg/mL (~763.59 mM)
|
|---|---|
| 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 | 3.0544 mL | 15.2718 mL | 30.5437 mL | |
| 5 mM | 0.6109 mL | 3.0544 mL | 6.1087 mL | |
| 10 mM | 0.3054 mL | 1.5272 mL | 3.0544 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
