AR420626是一种口服活性、选择性的游离脂肪酸受体3(FFAR3)激动剂，EC50值为2.2µM。
Cas No.:1798310-55-0
Sample solution is provided at 25 µL, 10mM.
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AR420626 is an oral active and selective agonist of free fatty acid receptor 3 (FFAR3) with an EC50 value of 2.2µM [1]. AR420626 increases the release of GLP-2 and stimulates HCO3− secretion via GLP-2 receptor activation [2]. AR420626 has been widely used to alleviate ulcer formation and gastrointestinal bleeding in rat models, and to protect gastrointestinal functions[3].
In vitro, AR420626 treatment for 48 hours significantly inhibited the proliferation of HepG2 cells, with an IC50 value of 25µM[4]. Treatment with 10µM AR420626 for 24 hours significantly enhanced the mRNA expression of TPH1 and SERT in RIN-14B cells, and also inhibited the level of IDO1[5]. Treatment with 20µM AR420626 for 24 hours significantly reduced the production of lipopolysaccharide-induced nitric oxide (NO) in RAW264.7 cells without affecting cell viability[6].
In vivo, AR420626 treatment via daily intraperitoneal injection at a dose of 26.64μg/kg for one week can improve glucose tolerance in streptozotocin (STZ)-induced diabetic mice and increase plasma insulin levels[7]. Daily oral administration of a 0.1mg/kg dose of AR420626 for 8 weeks prevented the motor disorders and loss of dopaminergic neurons in 6-hydroxydopamine (6-OHDA)-induced Parkinson's disease mice[8].
References:
[1] Lee Y J, Son S E, Im D S. Free fatty acid 3 receptor agonist AR420626 reduces allergic responses in asthma and eczema in mice[J]. International Immunopharmacology, 2024, 127: 111428.
[2] Iwasaki M, Akiba Y, Kaunitz J D. Duodenal chemosensing of short-chain fatty acids: implications for GI diseases[J]. Current gastroenterology reports, 2019, 21(8): 35.
[3] Mishra S P, Karunakar P, Taraphder S, et al. Free fatty acid receptors 2 and 3 as microbial metabolite sensors to shape host health: pharmacophysiological view[J]. Biomedicines, 2020, 8(6): 154.
[4] Mikami D, Kobayashi M, Uwada J, et al. AR420626, a selective agonist of GPR41/FFA3, suppresses growth of hepatocellular carcinoma cells by inducing apoptosis via HDAC inhibition[J]. Therapeutic advances in medical oncology, 2020, 12: 1758835920913432.
[5] Liu Z, Ling Y, Peng Y, et al. Regulation of serotonin production by specific microbes from piglet gut[J]. Journal of animal science and biotechnology, 2023, 14(1): 111.
[6] Salaga M, Bartoszek A, Binienda A, et al. Activation of free fatty acid receptor 4 affects intestinal inflammation and improves colon permeability in mice[J]. Nutrients, 2021, 13(8): 2716.
[7] Lee D H, Heo K S, Myung C S. Gαi‐coupled GPR41 activation increases Ca2+ influx in C2C12 cells and shows a therapeutic effect in diabetic animals[J]. Obesity, 2023, 31(7): 1871-1883.
[8] Hou Y, Shan C, Zhuang S, et al. Gut microbiota-derived propionate mediates the neuroprotective effect of osteocalcin in a mouse model of Parkinson’s disease[J]. Microbiome, 2021, 9(1): 34.
AR420626是一种口服活性、选择性的游离脂肪酸受体3(FFAR3)激动剂，EC50值为2.2µM[1]。AR420626可增加GLP-2的释放，并通过激活GLP-2受体刺激HCO3−分泌[2]。AR420626已被广泛用于减轻大鼠模型中的溃疡形成和胃肠道出血，并保护胃肠道功能[3]。
在体外，AR420626处理48小时显著抑制了HepG2细胞的增殖，IC50值为25µM[4]。10µM的AR420626处理RIN-14B细胞24小时，显著增强了TPH1和SERT的mRNA表达，同时也抑制了IDO1的水平[5]。20µM的AR420626处理RAW264.7细胞24小时，显著减少了脂多糖诱导的一氧化氮(NO)的产生，且不影响细胞活力[6]。
在体内，每日腹腔注射26.64µg/kg剂量的AR420626，持续一周，可改善链脲佐菌(STZ)诱导的糖尿病小鼠的葡萄糖耐量并增加血浆胰岛素水平[7]。每日口服0.1mg/kg剂量的AR420626，持续8周，可预防6-羟基多巴胺(6-OHDA)诱导的帕金森病小鼠的运动障碍和多巴胺能神经元丢失[8]。
| Cell experiment [1]: | |
Cell lines | HepG2 cells |
Preparation Method | HepG2 cells were grown in DMEM medium with 10% (v/v) fetal bovine serum (FBS), 100μg/ml streptomycin, and 100U/ml penicillin at 37°C in 5% CO2/atmosphere. HepG2 cells (5×103 cells) were seeded on 96-well plates, incubated for 24h, and then treated with different concentrations of AR420626 (0.1, 10, 25, and 50µM) at 37°C. After 48h, cell viability was measured. |
Reaction Conditions | 0.1, 10, 25, and 50µM; 48h |
Applications | AR420626 treatment significantly reduced the cell viability of HepG2 cells in a concentration-dependent manner. |
| Animal experiment [2]: | |
Animal models | ICR mice |
Preparation Method | Male ICR mice (4 weeks old) were housed singly in a standard environment with food and water ad libitum. Mice were acclimated for a week before starting the experiment. Mice were intraperitoneally administered with 50mg/kg of STZ in 0.1M sodium citrate buffer (pH 4.5) once a day for 2 days. Subsequently, AR420626 (26.64μg/kg) was intraperitoneally administered once a day for 7 days. Collect samples of mouse skeletal muscles for analysis. |
Dosage form | 26.64μg/kg/day for 7 days; i.p. |
Applications | AR420626 treatment significantly enhanced skeletal muscle glycogen storage in STZ-induced diabetic mice. |
References: | |
| Cas No. | 1798310-55-0 | SDF | |
| 化学名 | N-(2,5-dichlorophenyl)-4-(2-furanyl)-1,4,5,6,7,8-hexahydro-2-methyl-5-oxo-3-quinolinecarboxamide | ||
| Canonical SMILES | ClC1=CC(NC(C2=C(C)NC(CCCC3=O)=C3C2C4=CC=CO4)=O)=C(Cl)C=C1 | ||
| 分子式 | C21H18Cl2N2O3 | 分子量 | 417.3 |
| 溶解度 | 5mg/mL in DMSO, 2mg/mL in 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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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.3964 mL | 11.9818 mL | 23.9636 mL |
| 5 mM | 479.3 μL | 2.3964 mL | 4.7927 mL |
| 10 mM | 239.6 μL | 1.1982 mL | 2.3964 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。
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- Purity: >97.00% Appearance: A solid
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