1. GPCR/G Protein
  2. Free Fatty Acid Receptor
  3. GPR40 agonist 4

GPR40 agonist 4 是一个强效的游离脂肪酸受体 1 (FFA1/GPR40) 激动剂,其 pEC50 值为 7.54。

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GPR40 agonist 4 Chemical Structure

GPR40 agonist 4 Chemical Structure

CAS No. : 2102196-57-4

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10 mM * 1 mL in DMSO ¥1101
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Customer Review

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

GPR40 agonist 4 is a potent free fatty acid receptor 1 (FFA1/ GPR40) agonist with a pEC50 of 7.54.

IC50 & Target

pEC50: 7.54 (FFA1/GPR40)[1]

体外研究
(In Vitro)

GPR40 agonist 4 tends to have a low risk of activating caspase-3/7[1].

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

体内研究
(In Vivo)

Single oral administration of GPR40 agonist 4 (compound 20) robustly reduces the plasma glucose excursion and enhances insulin secretion during an oral glucose tolerance test (OGTT) in a dose-dependent manner from 1 to 10 mg/kg when GPR40 agonist 4 is dosed 60 min prior to the oral glucose challenge. The area under the curve of blood glucose (AUC0-120min) and blood insulin (AUC0-120min) reveal that the minimum effective dose of GPR40 agonist 4 is 3 mg/kg. The hyperglycemia state is also markedly improved in GPR40 agonist 4 (20 mg/kg) treated group[1].

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

分子量

416.87

Formula

C21H17ClO5S

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
In Vitro: 

DMSO 中的溶解度 : 160 mg/mL (383.81 mM; 超声加热助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.3988 mL 11.9941 mL 23.9883 mL
5 mM 0.4798 mL 2.3988 mL 4.7977 mL
查看完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献
Cell Assay
[1]

Human hepatocyte HepG2 cells are cultured at 37°C, 5% CO2 in DMEM supplemented with 10% fetal bovine serum, 50 μg/mL streptomycin and 50 IU/mL penicillin. Cells are seeded in a 96-well plate (2×104 cells/well) and cultured with GPR40 agonist 4 (compound 20) in DMEM for 24 h. FGPR40 agonist 4 is measured in three independent experiments[1].

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

Animal Administration
[1]

8 weeks old normal male SD rats after 1 week adaptation are fasted overnight (12 h), weighted, bled via the tail vein, and randomized into 5 groups (n=6 for each group). Rats are administrated orally with a single doses of vehicle (0.5% methylcellulose aqueous solution) or GPR40 agonist 4 (compound 20) (1, 3 and 10 mg/kg suspended in vehicle) and subsequently dosed orally with glucose aqueous solution (3 g/kg) after 60 min. Blood samples are collected immediately before drug administration (~60 min), before glucose challenge (0 min), and at 15, 30, 60 and 120 min post-dose. The blood glucose is measured by blood glucose test strips[1].

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

参考文献

GPR40 agonist 4 相关分类

完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3988 mL 11.9941 mL 23.9883 mL 59.9707 mL
5 mM 0.4798 mL 2.3988 mL 4.7977 mL 11.9941 mL
10 mM 0.2399 mL 1.1994 mL 2.3988 mL 5.9971 mL
15 mM 0.1599 mL 0.7996 mL 1.5992 mL 3.9980 mL
20 mM 0.1199 mL 0.5997 mL 1.1994 mL 2.9985 mL
25 mM 0.0960 mL 0.4798 mL 0.9595 mL 2.3988 mL
30 mM 0.0800 mL 0.3998 mL 0.7996 mL 1.9990 mL
40 mM 0.0600 mL 0.2999 mL 0.5997 mL 1.4993 mL
50 mM 0.0480 mL 0.2399 mL 0.4798 mL 1.1994 mL
60 mM 0.0400 mL 0.1999 mL 0.3998 mL 0.9995 mL
80 mM 0.0300 mL 0.1499 mL 0.2999 mL 0.7496 mL
100 mM 0.0240 mL 0.1199 mL 0.2399 mL 0.5997 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
GPR40 agonist 4
目录号:
HY-103083
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