FABPs ligand 6是一种FABP5和FABP7抑制剂，对FABP5和FABP7的Kd值分别为874nM和20nM。
Cas No.:2988135-14-2
Sample solution is provided at 25 µL, 10mM.
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FABPs ligand 6 is an FABP5 and FABP7 inhibitor with Kd values of 874nM and 20nM, respectively [1]. The FABPs ligand 6 can stabilize the mitochondrial membrane potential and reduce the release of pro-inflammatory cytokines IL-1β and TNF-α[2]. FABPs ligand 6 has been widely used to reduce cerebral ischemia-reperfusion injury in animals and to improve neurological deficits[3].
In vitro, FABPs ligand 6 treatment (10μM) for 48 hours inhibited the oligomerization/aggregation of α-synuclein in U251 cells and rescued cell death[4]. Treatment with 10μM FABPs ligand 6 for 48 hours significantly reduced the proliferation and migration of Skmel23 cells, and inhibited the activation of the Wnt/β-catenin signaling pathway[5].
In vivo, FABPs ligand 6 treatment via a single oral administration at a dose of 3mg/kg effectively reduced the brain infarction volume and neurological deficits 30minutes after cerebral ischemia-reperfusion in mice[3].
References:
[1] Cheng A, Jia W, Kawahata I, et al. A novel fatty acid-binding protein 5 and 7 inhibitor ameliorates oligodendrocyte injury in multiple sclerosis mouse models[J]. EBioMedicine, 2021, 72.
[2] Wu C, Lin J, Chen Q, et al. Targeting the FABP Axis: Interplay Between Lipid Metabolism, Neuroinflammation, and Neurodegeneration[J]. Cells, 2025, 14(19): 1502.
[3] Guo Q, Kawahata I, Degawa T, et al. Fatty acid-binding proteins aggravate cerebral ischemia-reperfusion injury in mice[J]. Biomedicines, 2021, 9(5): 529.
[4] Cheng A, Wang Y, Shinoda Y, et al. Fatty acid-binding protein 7 triggers α-synuclein oligomerization in glial cells and oligodendrocytes associated with oxidative stress[J]. Acta Pharmacologica Sinica, 2022, 43(3): 552-562.
[5] Umaru B A, Kagawa Y, Shil S K, et al. Ligand Bound Fatty Acid Binding Protein 7 (FABP7) Drives Melanoma Cell Proliferation Via Modulation of Wnt/β-Catenin Signaling: Umaru et al[J]. Pharmaceutical Research, 2021, 38(3): 479-490.
FABPs ligand 6是一种FABP5和FABP7抑制剂，对FABP5和FABP7的Kd值分别为874nM和20nM[1]。FABPs ligand 6能够稳定线粒体膜电位，并减少促炎细胞因子IL-1β和TNF-α的释放[2]。FABPs ligand 6已被广泛用于减轻动物脑缺血再灌注损伤并改善神经功能缺损[3]。
在体外，使用10μM的FABPs ligand 6处理U251细胞48小时，抑制了α-突触核蛋白的寡聚/聚集并挽救了细胞死亡[4]。使用10μM的FABPs ligand 6处理Skmel23细胞48小时，显著降低了细胞的增殖和迁移，并抑制了Wnt/β-连环蛋白信号通路的激活[5]。
在体内，单次口服3mg/kg剂量的FABPs ligand 6，在小鼠脑缺血再灌注后30分钟有效减少了脑梗死体积和神经功能缺损[3]。
| Cell experiment [1]: | |
Cell lines | U251 cells |
Preparation Method | U251 cells were grown in DMEM medium supplemented with 10% fetal bovine serum, 100U/ml penicillin, and 0.1mg/ml streptomycin in 5% CO2 at 37°C. The cells were treated with FABPs ligand 6 (1μM), antioxidant NAC (1μM), and arachidonic acid (AA) (100µM) for 48 hours, and then the cells were collected for Western blot (WB) analysis. |
Reaction Conditions | 1μM; 48h |
Applications | FABPs ligand 6 treatment significantly decreased the cleaved RIPK1 levels triggered by AA in U251 cells. |
| Animal experiment [2]: | |
Animal models | Male ICR mice |
Preparation Method | Male ICR mice (5 weeks old; 25-30g) were housed under conditions of constant temperature and humidity, kept on a 12-h light-dark cycle (lights on: 09:00–21:00) and fed ad libitum. Briefly, adult male ICR mice were anesthetized via intraperitoneal injection with a combination of 0.3mg/kg medetomidine, 4.0mg/kg midazolam and 5.0mg/kg butorphanol. transient middle cerebral artery occlusion (tMCAO) surgical procedure was performed as follows: a silicone-coated 6-0 suture was inserted from the right external carotid artery to the internal carotid artery, extending to the origin of a middle cerebral artery, for 2h. After 2h, the suture was removed, allowing reperfusion to occur. Mice in the sham-operation group underwent the same procedure, except for the suture insertion. A homoeothermic heating blanket was used to the maintain core body temperature in each mouse at 37°C during the I/R operation. Regional cerebral blood flow (rCBF) was monitored by laser-doppler flowmetry to confirm whether the right hemisphere was in an ischemic state. FABPs ligand 6 was suspended in 0.5% carboxymethyl cellulose (CMC) and administered (p.o.) at 3mg/kg 30min after reperfusion. The brains were collected for analyses. |
Dosage form | 3mg/kg for once; p.o. |
Applications | FABPs ligand 6 treatment reduced infarct volumes in mice. |
References: | |
| Cas No. | 2988135-14-2 | SDF | Download SDF |
| 别名 | MF6 | ||
| 分子式 | C28H27FN2O3 | 分子量 | 458.52 |
| 溶解度 | DMSO : 250 mg/mL (545.23 mM; Need ultrasonic) | 储存条件 | 4°C, protect from light |
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1809 mL | 10.9046 mL | 21.8093 mL |
| 5 mM | 436.2 μL | 2.1809 mL | 4.3619 mL |
| 10 mM | 218.1 μL | 1.0905 mL | 2.1809 mL |
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动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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2.
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