产品
编 号:F137327
分子式:C19H25N3O4
分子量:359.42
产品类型
结构图
CAS No: 1359963-68-0
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产品详情
生物活性:
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.
体内研究:
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.The pharmacokinetic parameters of FEMA 4774 (S9632) in Male and Female Sprague-Dawley Rats RouteDayDose (mg/kg)SexCmax (ng/mL)±SDTmax (hr)t1/2 (hr)AUC0last(ng?hr/mL)AUC0last/dose(ng?hr/mL/mg/kg)%F
iv11.0M2036.7±281.90.030.19330.6±58330.6-
F2625.8±679.90.030.27411.9±116.3411.9-
Oral gavage110M12.9±3.20.251.2117.9±2.31.790.54
F34.0±3.90.251.1749.2±7.84.921.19
30M90.0±23.90.330.8890.8±11.03.030.92
F62.4±25.90.421.0695.0±20.43.170.77
100M147.2±86.30.330.71176.2±73.81.760.53
F268.5±90.70.250.99341.1±81.03.410.83
Oral gavage710M16.2±3.60.500.8448.1±33.24.81-
F32.7±9.70.331.1758.9±25.45.89-
30M74.5±16.20.330.9486.0±8.72.87-
F77.1±41.70.251.39106.8±8.73.56-
100M117.9±15.30.250.72185.3±15.31.85-
F189.7±79.50.250.89278.9±79.02.79-
体外研究:
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.