5-PAHSA
目录号 : GC403225-PAHSA是一种脂肪酸脂肪酸酯（Fatty Acid Esters of Fatty Acids, FAHFAs） 家族中的重要成员，这个家族是一类新发现的内源性脂质分子。5-PAHSA能够改善葡萄糖稳态和胰岛素敏感性，具有强效抗糖尿病和抗炎特性。
Cas No.:1481636-41-2
Sample solution is provided at 25 µL, 10mM.
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5-PAHSA is an important member of the fatty acid esters of fatty acids (FAHFAs) family, a recently discovered class of endogenous lipid molecules[1]. 5-PAHSA improves glucose homeostasis and insulin sensitivity, exhibiting potent anti-diabetic and anti-inflammatory properties[2, 3]. 5-PAHSA is naturally present in human and animal adipose tissue, liver, and blood, with its levels influenced by factors such as diet, insulin sensitivity, and genetic background[4].
In vitro, 5-PAHSA (30μM) treatment of PC12 cells for 24h reduced intracellular reactive oxygen species (ROS) levels, increased C-reactive protein (CRP) levels, and induced autophagy[5]. Treatment of HepG2 and 3T3-L1 cells with 5-PAHSA (20μM) for 2 days significantly reduced insulin resistance induced by high insulin and TNF-α, improving glucose uptake and insulin signaling[6].
In vivo, oral administration of 5-PAHSA (50 or 150mg/kg/day) to db/db mice for 30 days significantly reduced serum oxidized low-density lipoprotein (ox-LDL) levels and the phosphorylation level of mTOR protein at Ser2448 in the cerebral cortex[5].
References:
[1] Aryal P, Syed I, Lee J, et al. Distinct biological activities of isomers from several families of branched fatty acid esters of hydroxy fatty acids (FAHFAs)[J]. Journal of lipid research, 2021, 62: 100108.
[2] Yore M M, Syed I, Moraes-Vieira P M, et al. Discovery of a class of endogenous mammalian lipids with anti-diabetic and anti-inflammatory effects[J]. Cell, 2014, 159(2): 318-332.
[3] Pflimlin E, Bielohuby M, Korn M, et al. Acute and repeated treatment with 5-PAHSA or 9-PAHSA isomers does not improve glucose control in mice[J]. Cell metabolism, 2018, 28(2): 217-227. e13.
[4] Kang Z, Jin Z, Wu L, et al. Investigating the Pathogenesis and Treatment of Type 2 Diabetes from the Perspective of Adipose Tissue[J]. Diabetes, Metabolic Syndrome and Obesity, 2025: 2343-2360.
[5] Wang J, Yu Z, Tao Y, et al. A novel palmitic acid hydroxy stearic acid (5‐PAHSA) plays a neuroprotective role by inhibiting phosphorylation of the m‐TOR‐ULK1 pathway and regulating autophagy[J]. CNS neuroscience & therapeutics, 2021, 27(4): 484-496.
[6] Wang Y M, Liu H X, Fang N Y. High glucose concentration impairs 5-PAHSA activity by inhibiting AMP-activated protein kinase activation and promoting nuclear factor-kappa-B-mediated inflammation[J]. Frontiers in pharmacology, 2019, 9: 1491.
5-PAHSA是一种脂肪酸脂肪酸酯（Fatty Acid Esters of Fatty Acids, FAHFAs） 家族中的重要成员，这个家族是一类新发现的内源性脂质分子[1]。5-PAHSA能够改善葡萄糖稳态和胰岛素敏感性，具有强效抗糖尿病和抗炎特性[2, 3]。5-PAHSA在人体和动物的脂肪组织、肝脏和血液中天然存在，其水平受饮食、胰岛素敏感性和遗传背景等因素影响[4]。
在体外，5-PAHSA（30µM）处理PC12细胞24h，降低了细胞内活性氧（ROS）水平，升高了C反应蛋白（CRP）水平，诱导了细胞自噬[5]。5-PAHSA（20µM）处理HepG2细胞和3T3-L1细胞2天，显著降低了高胰岛素和TNF-α诱导的胰岛素抵抗，改善了细胞的葡萄糖摄取和胰岛素信号转导[6]。
在体内，5-PAHSA（50, 150mg/kg/day）通过口服处理DB/DB小鼠30天，显著降低了小鼠血清中氧化型低密度脂蛋白（ox-LDL）的水平，也显著降低了大脑皮层中mTOR蛋白在Ser2448位点的磷酸化水平[5]。
| Cell experiment [1]: | |
Cell lines | PC12 cells |
Preparation Method | Cells were cultured separately in 4 types of medium, including Dulbecco's modified eagle medium (DMEM) high glucose, DMEM with extra glucose and fatty acid (GF, glucose 100mM, fatty acid 250μM), GF+DMSO, and GF+5-PAHSA (30μM). Cells were cultured in an incubator at 37°C and 5% CO2 for 24h. Detection of reactive oxygen species (ROS). |
Reaction Conditions | 30µM; 24h |
Applications | Under diabetic conditions, treatment of PC12 cells with 5-PAHSA can activate the autophagy process and reduce the level of reactive oxygen species (ROS) within the cells. |
| Animal experiment [1]: | |
Animal models | DB/DB mice、C57BL/6 mice |
Preparation Method | Male DB/DB mice (40 weeks-of-age) were used to create an animal model of type 2 diabetes; male C57BL/6 mice of the same age were used as controls. Mice were maintained on a 12-h light/dark cycle and had free access to food and water. Mice from each group were divided into 3 groups (n=6-8 per group), including a vehicle group (sodium carboxymethyl cellulose), a low-dose group (50mg/kg 5-PAHSA), and a high-dose group (150mg/kg 5-PAHSA). Animals were administered with these doses once daily by oral gavage. Fasting blood glucose levels were measured before and at 10 and 30 days after administration. After 30 days of drug administration, the animals were sacrificed in order to harvest organs and collect blood samples. |
Dosage form | 50, 150mg/kg/day; 30 days; p.o. |
Applications | Fasting blood glucose, glucose tolerance, and plasma insulin did not improve significantly after 30 days of 5-PAHSA administration; however, ox-LDL was significantly lower in DB/DB mice. The phosphorylation of m-TOR at Ser2448 was suppressed in the cortex of DB/DB mice after 30 days of 5-PAHSA administration. |
References: | |
| Cas No. | 1481636-41-2 | SDF | |
| Canonical SMILES | OC(CCCC(OC(CCCCCCCCCCCCCCC)=O)CCCCCCCCCCCCC)=O | ||
| 分子式 | C34H66O4 | 分子量 | 538.9 |
| 溶解度 | DMF: 20 mg/ml,DMSO: 15 mg/ml,Ethanol: 20 mg/ml,Ethanol:PBS(pH 7.2) (1:1): 0.5 mg/ml | 储存条件 | Store at -20°C |
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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 | 1.8556 mL | 9.2782 mL | 18.5563 mL |
| 5 mM | 371.1 μL | 1.8556 mL | 3.7113 mL |
| 10 mM | 185.6 μL | 927.8 μL | 1.8556 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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Quality Control & SDS
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- Purity: >95.00%
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