FEMA 4774

立即咨询

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。

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 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	C_max(ng/mL)±SD	T_max(hr)	t_1/2(hr)	AUC0_last(ng•hr/mL)	AUC0_last/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	-