AH 7614
(Synonyms: NSC 31171，N-xanthen-9-yl-p-Toluenesulfonamide) 目录号 : GC17753A selective FFAR4 antagonist
Cas No.:6326-06-3
Sample solution is provided at 25 µL, 10mM.
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Target: FFA4/GPR120
IC50: N/A
AH7614 is a selective and potent free fatty acid receptor 4 (FFA4/GPR120) antagonist with pIC50 values of 7.1, 8.1 and 8.1 at the human, mouse and rat receptor, respectively [1]. The free fatty acid receptor 4 (FFA4/GPR120), a member of the G protein-coupled receptor family, is a potential 7TM receptor involved in long-chain fatty acid-stimulated glucagon-like peptide-1 (GLP-1) secretion. FFA4 is highly expressed in the intestinal endocrine cell line STC-1 and the intestine. GLP-1 regulates multiple physiological functions including eating behavior [2].
In vitro: AH7614 (0.063, 0.25, and 1μM) blocked linoleic acid and GSK137647A-induced intracellular calcium increase in U2OS osteosarcoma cells expressing the FFA4 receptor [1]. In addition, the increase of glucose-stimulated insulin secretion by GSK137647A (50 μM) was abolished in the presence of the selective FFA4 antagonist AH7614 (100 μM) in the MIN6 mouse insulinoma cell line. Moreover, AH7614 (100 μM) blocked GSK137647A (100μM)-mediated a modest increase of GLP-1 secretion in the NCIH716 cells [1].
In vivo: N/A
References:
1. Sparks SM, Chen G, Collins JL, Danger D, Dock ST, Jayawickreme C, et al. Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120). Bioorg Med Chem Lett. 2014;24(14):3100-3.
2. Martin C, Passilly-Degrace P, Chevrot M, Ancel D, Sparks SM, Drucker DJ, et al. Lipid-mediated release of GLP-1 by mouse taste buds from circumvallate papillae: putative involvement of GPR120 and impact on taste sensitivity. J Lipid Res. 2012;53(11):2256-65.
| Cell experiment [1]: | |
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Cell lines |
Flp-In T-REx 293 cells |
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Preparation method |
The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
10-10 ~10-5 M for 15 minutes |
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Applications |
AH-7614 inhibited, in a potent and concentration-dependent manner, the ability of ω-3 fatty acid aLA to promote Ca2+ mobilization in Flp-In T-REx 293 cells induced to express hFFA4-eYFP. As an antagonist of FFA4, AH-7614 is able to block effects of both the polyunsaturated ω-6 fatty acid linoleic acid |
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References: [1] Watterson KR, Hansen SVF, Hudson BD, et al. Probe-Dependent Negative Allosteric Modulators of the Long-Chain Free Fatty Acid Receptor FFA4. Mol Pharmacol. 2017 Jun;91(6):630-641. |
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| Cas No. | 6326-06-3 | SDF | |
| 别名 | NSC 31171，N-xanthen-9-yl-p-Toluenesulfonamide | ||
| 化学名 | 4-methyl-N-(9H-xanthen-9-yl)benzenesulfonamide | ||
| Canonical SMILES | O=S(NC1C2=C(C=CC=C2)OC3=CC=CC=C31)(C4=CC=C(C)C=C4)=O | ||
| 分子式 | C20H17NO3S | 分子量 | 351.42 |
| 溶解度 | 30mg/mL in DMSO & DMF | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.8456 mL | 14.228 mL | 28.456 mL |
| 5 mM | 0.5691 mL | 2.8456 mL | 5.6912 mL |
| 10 mM | 0.2846 mL | 1.4228 mL | 2.8456 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet