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AH-7614

目录号: PL04999 纯度: ≥99%

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。

CAS No. :6326-06-3

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中文名称	AH-7614
英文名称	AH-7614
英文别名	Benzenesulfonamide,4-methyl-N-9H-xanthen-9-yl-;AH 7614;4-Methyl-N-(9H-xanthen-9-yl)-benzenesulfonamide;4-methyl-N-9H-xanthen-9-yl-Benzamide;N-(9-xanthyl)-4-toluensulfonamide;N-(9-Xanthyl)-p-toluamid;N-(9-xanthyl)-p-toluensulfonamide;N-xanthen-9-yl-p-toluamide;N-xanthen-9-yl-toluene-4-sulfonamide;N-Xanthen-9-yl-toluol-4-sulfonamid;N-xanthyl-p-toluenesulfonamide;4-Methyl-N-9H-xanthen-9-yl-benzenesulfonamide;Compound 39;NSC 31171;p-Toluenesulfonamide, N-xanthen-9-yl-;4-Methyl-N-(9H-xanthen-9-yl)benzenesulfonamide;AH7614;p-Toluenesulfonamide, N-(xanthen-9-yl)-;N-Tosyl-9H-xanthene-9-amine;NSC31171;ChemDiv3_003436;Oprea1_006107;Oprea1_382032;4-methyl-N-(9H-xanthen-9-yl)benzene-1-sulfonamide;HMS1482M04;BDBM50044874;s9477;STK325647;CCG-
Cas No.	6326-06-3
分子式	C₂₀H₁₇NO₃S
分子量	351.42
包装储存	Powder -20°C 3 years；4°C 2 years
详情描述	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。

产品详情	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 selective FFA4 (GPR120) antagonist, with pIC 50 s of 7.1, 8.1, and 8.1 for human, mouse, and rat FFA4, respectively. AH-7614 has selectivity for FFA4 over FFA1 (pIC 50 <4.6). AH-7614 is able to block effects of both the polyunsaturated ω-6 fatty acid linoleic acid and the synthetic FFA4 agonist.
性状	Solid
IC50 & Target[1][2]	pIC50: 7.1 (human FFA4)
体外研究(In Vitro)	AH-7614 (compound 39) (0.063-1 μM) blocks intracellular Ca response induced by both linoleic acid and FFAR4 agonist in FFA4 expressing U2OS cells. AH-7614 (100 μM) abolishes the enhancement in glucose-stimulated insulin secretion by GSK137647A in NCI-H716 cells. AH-7614 (0.001-10 μM; 15 min) blocks TUG-891-mediated internalization of FFA4 from the cell surface (pIC50=7.70). AH-7614 (10 μM; 30 min) blocks agonist-induced elevation of intracellular inositol monophosphates and phosphorylation of FFA4. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	AH7614 (50?μg; intratumoral injection once every 4?d for 20 d) reduces the tumor growth in mice. 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. has not independently confirmed the accuracy of these methods. They are for reference only.
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
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.

溶解度数据	In Vitro: DMSO : 100 mg/mL (284.56 mM; Need ultrasonic)配制储备液

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[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.

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

AH-7614

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