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

GPR40 agonist 4 

目录号: HY-103083 纯度: 98.69%
产品使用指南

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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  • 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
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 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 160 mg/mL (383.81 mM; Need ultrasonic and warming)

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
10 mM 0.2399 mL 1.1994 mL 2.3988 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。-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。

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
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2

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GPR40 agonist 4
目录号:
HY-103083
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