FEMA 4774|cas:1359963-68-0|西域试剂

FEMA 4774,99.85%

产品编号：Bellancom-139091| CAS NO：1359963-68-0| 分子式：C₁₉H₂₅N₃O₄| 分子量：359.42

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货号	价格	库存与货期
Bellancom-139091	￥1800.00	杭州北京（现货）
Bellancom-139091	￥2800.00	杭州北京（现货）
Bellancom-139091	￥5200.00	杭州北京（现货）
Bellancom-139091	￥8000.00	杭州北京（现货）
Bellancom-139091	￥12000.00	杭州北京（现货）

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FEMA 4774

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。

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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

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	-

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

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	-

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

性状

Solid

溶解性数据

In Vitro:

DMSO : ≥ 41.67 mg/mL (115.94 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.7823 mL	13.9113 mL	27.8226 mL
5 mM	0.5565 mL	2.7823 mL	5.5645 mL
10 mM	0.2782 mL	1.3911 mL	2.7823 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

参考文献