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AH-7614 98%

货号:A834543 同义名: NSC 31171;N-xanthen-9-yl-p-Toluenesulfonamide 产品仅供科研

AH 7614 is a selective free fatty acid receptor 4 (FFA4/GPR120) antagonist with pIC50 of 7.1 for human FFA4.

AH-7614 化学结构 CAS号:6326-06-3
AH-7614 化学结构
CAS号:6326-06-3
AH-7614 3D分子结构
CAS号:6326-06-3
AH-7614 化学结构 CAS号:6326-06-3
AH-7614 3D分子结构 CAS号:6326-06-3
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AH-7614 纯度/质量文件

货号:A834543 标准纯度:98%
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AH-7614 生物活性

描述 AH-7614 demonstrates potent and selective antagonism against FFA4 (GPR120), with pIC50 values of 7.1, 8.1, and 8.1 for human, mouse, and rat FFA4, respectively. It exhibits selectivity for FFA4 over FFA1 (pIC50<4.6). AH-7614 effectively inhibits the actions of both the polyunsaturated ω-6 fatty acid linoleic acid and the synthetic FFA4 agonist[1].[2]. AH-7614 (0.063-1 μM) inhibits the intracellular Ca2+ response induced by both linoleic acid and FFAR4 agonist in FFA4 expressing U2OS cells[1]. AH-7614 (100 μM) eliminates the enhancement in glucose-stimulated insulin secretion by GSK137647A in NCI-H716 cells[1]. AH-7614 (0.001-10 μM; 15 min) prevents TUG-891-mediated internalization of FFA4 from the cell surface (pIC50=7.70)[2]. AH-7614 (10 μM; 30 min) inhibits agonist-induced elevation of intracellular inositol monophosphates and phosphorylation of FFA4[2].

AH-7614 动物研究

Animal study AH7614 (50 μg; intratumoral injection once every 4 days for 20 days) decreases tumor growth in mice[3]. AH7614 (50 μg; intratumoral injection one day prior to epirubicin injection) enhances cancer cell sensitivity to chemotherapy and inhibits tumor progression by blocking GPR120 signaling in combination with Epirubicin[3].

AH-7614 参考文献

[1]Sparks SM, et, al. Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120). Bioorg Med Chem Lett. 2014 Jul 15;24(14):3100-3.

[2]Watterson KR, et, al. Probe-Dependent Negative Allosteric Modulators of the Long-Chain Free Fatty Acid Receptor FFA4. Mol Pharmacol. 2017 Jun;91(6):630-641.

[3]Wang X, et, al. Fatty acid receptor GPR120 promotes breast cancer chemoresistance by upregulating ABC transporters expression and fatty acid synthesis. EBioMedicine. 2019 Feb;40:251-262.

AH-7614 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.85mL

0.57mL

0.28mL

14.23mL

2.85mL

1.42mL

28.46mL

5.69mL

2.85mL

AH-7614 技术信息

CAS号6326-06-3
分子式C20H17NO3S
分子量351.419
别名 NSC 31171;N-xanthen-9-yl-p-Toluenesulfonamide
运输蓝冰
存储条件

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 105 mg/mL(298.79 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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