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FEMA 4774
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
FEMA 4774图片
CAS NO:1359963-68-0
包装与价格:
包装价格(元)
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
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 tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation 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

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-