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| Targets |
FEMA 4774 targets the T1R2 and T1R3 subunits of the human sweet taste receptor, a G protein-coupled receptor complex responsible for sweet taste perception. As a positive allosteric modulator, FEMA 4774 binds to a site distinct from the orthosteric binding site of sweeteners and enhances the receptor's response to sucrose and other sweeteners. This mechanism allows FEMA 4774 to act as a sucrose sweetness enhancer, reducing the amount of sugar needed to achieve the desired sweetness in food products.
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| ln Vitro |
FEMA 4774 (0-50 μM) greatly increases sucrose's affinity to its binding site and causes a dose-dependent drop in sucrose EC50 values. In human sweet taste receptors, 30 cells, the α (modulator influence on agonist affinity) values are affected[1].
In vitro studies demonstrate that FEMA 4774 acts as a positive allosteric modulator of the T1R2/T1R3 sweet taste receptor. Its activity can be assessed using cell-based assays in which cells expressing the human sweet taste receptor are treated with FEMA 4774 in the presence of sucrose or other sweeteners. The compound's ability to enhance sweet taste receptor activation is measured by quantifying receptor-mediated signaling, such as calcium mobilization or cAMP accumulation. |
| ln Vivo |
In Swiss albino (CD-1) mice, oral gavage administered at doses ranging from 500-2000 mg/kg did not result in a dose-dependent rise in polychromatic erythrocytes; nevertheless, it did trigger the development of micronuclei. 2]. Pharmacokinetic Parameters of FEMA 4774 (S9632) in Male and Female Sprague-Dawley Rats Route Daily Dose (mg/kg) Sex Cmax (ng/mL)±SD Tmax (hr) t1/2 (hr) AUC0last( ng·hr/ mL) AUC0last/dose (ng·hr/mL/mg/kg) %F iv 1 1.0 M 2036.7±281.9 0.03 0.19 330.6±58 330.6 - F 2625.8±679.9 0.03 0.27 411.9±116.3 411.9 - Oral gavage 1 10 meters 12.9± 3.2 0.25 1.21 17.9±2.3 1.79 0.54F 34.0±3.9 0.25 1.17 49.2±7.8 4.92 1.19 30M 90.0±23.9 0.33 0.88 90.8±11.0 3.03 0 .92F 62.4±2 5.9 0.42 1.06 95.0±20.4 3.17 0.77 100M 147.2± 86.3 0.33 0.71 176.2 ±73.8 1.76 0.53 F 268.5±90.7 0.25 0.99 341.1±81.0 3.41 0.83 Oral gavage 7 10 M 16.2±3.6 0.50 0.84 48.1±33.2 4.81 - F 32.7±9.7 0.33 1.17 58.9±25.4 5.89 - 30M 74.5±16.2 0.33 0.94 86.0± 8.7 2.87 - F 77.1±41.7 0.25 1.39 106.8±8.7 3.56 - 100 M 117.9±15.3 0.25 0.72 185.3±15.3 1.85
FEMA 4774 shows obvious enhancement of the sweetness of sucrose in sensory evaluation tests. In these tests, trained human panelists evaluate the sweetness intensity of sucrose solutions with and without the addition of FEMA 4774. The compound significantly increases the perceived sweetness of sucrose, demonstrating its efficacy as a sweetness enhancer. FEMA 4774 is used in the food and beverage industry to reduce sugar content while maintaining sweetness. |
| Enzyme Assay |
Sensory evaluation tests for FEMA 4774 are conducted using trained human panelists to assess its sweetness-enhancing effects. Panelists evaluate the sweetness intensity of sucrose solutions containing varying concentrations of FEMA 4774 compared to sucrose-only controls. The compound's ability to enhance sweetness is quantified using a rating scale or by determining the equivalent sucrose concentration. These tests are conducted under controlled conditions to ensure reproducibility and accuracy.
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| Cell Assay |
In vitro cellular assays for FEMA 4774 involve treating cells expressing the human sweet taste receptor T1R2/T1R3 with the compound and measuring receptor activation. Cells are loaded with a calcium-sensitive dye (e.g., Fluo-4) and treated with varying concentrations of FEMA 4774 in the presence of a fixed concentration of sucrose or other sweetener. The increase in intracellular calcium concentration is measured using a fluorescence plate reader. The EC50 for potentiation of the sweetener response is determined from dose-response curves.
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| Animal Protocol |
In vivo animal experiments are not applicable for FEMA 4774 as it is a flavoring agent and sweetness enhancer used in food products, not a therapeutic agent. Its safety and efficacy are evaluated through sensory evaluation tests in humans and through toxicological studies conducted according to JECFA guidelines. The compound is not administered to animals for pharmacological studies.
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| ADME/Pharmacokinetics |
FEMA 4774 has a molecular weight of 359.42 and a molecular formula of C19H25N3O4. It is a white to off-white solid powder at room temperature. The compound is soluble in DMSO (250 mg/mL, ultrasonic). Purity is typically >99%. It is stable under recommended storage conditions and is protected from light and moisture.
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| Toxicity/Toxicokinetics |
FEMA 4774 has been evaluated by JECFA and is considered to have no safety concern at current levels of intake when used as a flavoring agent. The compound is generally recognized as safe for use in food products at the levels typically employed for sweetness enhancement. Standard food safety precautions should be followed when handling the compound.
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| References | |
| Additional Infomation |
FEMA 4774 (CAS 1359963-68-0) is a positive allosteric modulator of the T1R2/T1R3 sweet taste receptor and a sucrose sweetness enhancer. It shows obvious enhancement of the sweetness of sucrose in sensory evaluation tests. The compound has been evaluated by JECFA and is considered to have no safety concern at current levels of intake when used as a flavoring agent. FEMA 4774 is used in the food and beverage industry to reduce sugar content while maintaining sweetness.
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| Molecular Formula |
C19H25N3O4
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| Molecular Weight |
359.426
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| Exact Mass |
359.184
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| CAS # |
1359963-68-0
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| PubChem CID |
66746559
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
602.1±55.0 °C at 760 mmHg
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| Flash Point |
318.0±31.5 °C
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| Vapour Pressure |
0.0±1.8 mmHg at 25°C
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| Index of Refraction |
1.602
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| LogP |
3.48
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
26
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| Complexity |
523
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
RHXLOOCFQPJWBW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H25N3O4/c1-10(2)21-18(25)19(4,5)9-26-13-8-6-7-12-15(13)16(20)14(17(23)24)11(3)22-12/h6-8,10H,9H2,1-5H3,(H2,20,22)(H,21,25)(H,23,24)
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| Chemical Name |
4-amino-5-[2,2-dimethyl-3-oxo-3-(propan-2-ylamino)propoxy]-2-methylquinoline-3-carboxylic acid
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| Synonyms |
FEMA 4774; FEMA-4774; FEMA4774
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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: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 : ≥ 41.67 mg/mL (~115.94 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 | 2.7822 mL | 13.9109 mL | 27.8218 mL | |
| 5 mM | 0.5564 mL | 2.7822 mL | 5.5644 mL | |
| 10 mM | 0.2782 mL | 1.3911 mL | 2.7822 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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