AH-7614 是一种有效和选择性的FFA4 (GPR120)拮抗剂,对人,小鼠和大鼠 FFA4 的pIC50值分别为 7.1,8.1 和 8.1。AH-7614 对 FFA4 的选择性高于 FFA1 (pIC50<4.6)。AH-7614 能够阻断多不饱和 ω-6 脂肪酸亚油酸和 FFA4 激动剂的作用。
生物活性 | AH-7614 is a potent and selectiveFFA4 (GPR120)antagonist, withpIC50s of 7.1, 8.1, and 8.1 for human, mouse, and rat FFA4, respectively. AH-7614 has selectivity for FFA4 over FFA1 (pIC50<4.6). AH-7614 is able to block effects of both the polyunsaturated ω-6 fatty acid linoleic acid and the synthetic FFA4 agonist[1][2]. |
IC50& Target | pIC50: 7.1 (human FFA4)[1] |
体外研究 (In Vitro) | AH-7614 (compound 39) (0.063-1 μM) blocks intracellular Ca2+response induced by both linoleic acid and FFAR4 agonist in FFA4 expressing U2OS cells[1]. AH-7614 (100 μM) abolishes the enhancement in glucose-stimulated insulin secretion by GSK137647A in NCI-H716 cells[1]. AH-7614 (0.001-10 μM; 15 min) blocks TUG-891-mediated internalization of FFA4 from the cell surface (pIC50=7.70)[2]. AH-7614 (10 μM; 30 min) blocks agonist-induced elevation of intracellular inositol monophosphates and phosphorylation of FFA4[2].
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体内研究 (In Vivo) | AH7614 (50 μg; intratumoral injection once every 4 d for 20 d) reduces the tumor growth in mice[3]. AH7614 (50 μg; intratumoral injection one day prior to epirubicin injection) enhances cancer cell sensitivity to the chemotherapy and inhibit tumor progression by blocking GPR120 signaling in combination with Epirubicin[3].
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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 |
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溶解性数据 | In Vitro: DMSO : 100 mg/mL(284.56 mM;Need ultrasonic) 配制储备液 1 mM | 2.8456 mL | 14.2280 mL | 28.4560 mL | 5 mM | 0.5691 mL | 2.8456 mL | 5.6912 mL | 10 mM | 0.2846 mL | 1.4228 mL | 2.8456 mL |
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