FEMA 4774 是味觉受体 T1R2 和 T1R3 的正变构调节剂，其中 T1R2 和 T1R3 是人类甜味受体的两个亚基。FEMA 4774 也可作为蔗糖甜味增强剂。
| Cas No. | 1359963-68-0 |
| 分子式 | C19H25N3O4 |
| 分子量 | 359.42 |
| 溶解度 | DMSO : ≥ 41.67 mg/mL (115.94 mM) |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | FEMA 4774 is a positive allosteric modulator of taste receptorsT1R2andT1R3, 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 EC50value 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 | - | |
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