FEMA 4774 |
Catalog No.GC66047
One-Click Copy Product Info
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FEMA 4774 is a positive allosteric modulator of taste receptors T1R2 and T1R3, two subunits of the human sweet taste receptor. FEMA 4774 is also used as a sucrose sweetness enhancer.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1359963-68-0
Sample solution is provided at 25 µL, 10mM.
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FEMA 4774 is a positive allosteric modulator of taste receptors T1R2 and T1R3, two subunits of the human sweet taste receptor. FEMA 4774 is also used as a sucrose sweetness enhancer[1].
FEMA 4774 (0-50 μM) induces a dose-dependent decrease in the EC50 value of sucrose and significantly enhances the affinity of sucrose for its binding site with an α (effect of modulator on agonist affinity) value of 30 in the human sweet receptor cells[1].
FEMA 4774 (S9632) (oral gavage, 500-2000 mg/kg) does not cause a dose-dependent increase in polychromatic erythrocytes and induces micronuclei formation at dose levels up to 2000 mg/kg in Swiss albino (CD-1) mice[2].
The pharmacokinetic parameters of FEMA 4774 (S9632) in Male and Female Sprague-Dawley Rats
| Route | Day | 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 | M | 12.9±3.2 | 0.25 | 1.21 | 17.9±2.3 | 1.79 | 0.54 |
| F | 34.0±3.9 | 0.25 | 1.17 | 49.2±7.8 | 4.92 | 1.19 | |||
| 30 | M | 90.0±23.9 | 0.33 | 0.88 | 90.8±11.0 | 3.03 | 0.92 | ||
| F | 62.4±25.9 | 0.42 | 1.06 | 95.0±20.4 | 3.17 | 0.77 | |||
| 100 | M | 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 | - | |||
| 30 | M | 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 | - | ||
| F | 189.7±79.5 | 0.25 | 0.89 | 278.9±79.0 | 2.79 | - | |||
| Cas No. | 1359963-68-0 | SDF | |
| Formula | C19H25N3O4 | M.Wt | 359.42 |
| Solubility | DMSO : ≥ 41.67 mg/mL (115.94 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.7823 mL | 13.9113 mL | 27.8226 mL |
| 5 mM | 556.5 μL | 2.7823 mL | 5.5645 mL |
| 10 mM | 278.2 μL | 1.3911 mL | 2.7823 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)