Epalrestat 是一种醛糖还原酶抑制剂，用于治疗糖尿病性神经病变 | MedChemExpress (MCE)

参考详情：Epalrestat (ONO2235，依帕司他) - 仅供科研 | 醛糖还原酶抑制剂 | MCE

中文名：依帕司他

CAS：82159-09-9

品牌：MedChemExpress (MCE)

存储条件：-20°C, protect from light

生物活性：Epalrestat 是一种醛糖还原酶抑制剂，用于治疗糖尿病性神经病变。目标：醛糖还原酶依帕司他可能影响或延缓潜在疾病进程的进展。评估了来自六项临床试验的数据，并确定与基线和安慰剂相比，依帕司他 50 mg 3 次/天可以改善运动和感觉神经传导速度和主观神经病变症状。依帕司他可作为一种新的治疗选择来预防或减缓糖尿病性神经病变的进展 [1]。 Epalrestat 显着增加了 EGG 上 3 cpm 波的振幅，并改善了心率变异性的光谱分析参数。这些发现表明依帕司他可用于治疗糖尿病性胃轻瘫 [2]。依帕司他是治疗糖尿病性神经病变的高效且安全的药物[3]。

体外：Epalrestat (100 和 200 µM，24 小时) 可抑制大鼠雪旺细胞 (SC) 中的细胞活力并诱导细胞凋亡[5]。Epalrestat (10 和 50 µM，24 小时) 通过 Nrf2 激活上调 γ-GCS，从而增加大鼠 SC 中的细胞内谷胱甘肽水平[5]。 Epalrestat (50 µM，16 小时) 可保护 SC 免受氧化应激[5]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内：Epalrestat (0.08% (w/w), 在常规饲料中, 8 周) 显示出对 db/db 小鼠糖尿病肾病的肾炎保护作用[4]。 Epalrestat (100 mg/kg 每日, i.g., 持续 6 周) 在 Streptozotocin (链脲佐菌素 (HY-13753)) 诱导的糖尿病周围神经病变 (DPN) 模型中可保护大鼠免受糖尿病周围神经损伤[6]。 Epalrestat (50 mg/kg, 口服灌胃, 每天两次) 可减少小鼠脑缺血引起的梗塞体积和血脑屏障通透性[7]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: db/db mice[4] Dosage: 0.08% (w/w) in fed regular chow Administration: 8 weeks Result: Ameliorated GBM thickening and mesangial matrix deposition in kidney tissue. Reduced the elevated sorbitol and fructose in the plasma, urine, and renal cortex of db/db mice. Reduced myo-inositol in the plasma and urine, whereas increased myo-inositol in the renal cortex. Animal Model: Rats were treated with high-fat and high-sugar diet for 4 weeks, and injected with Streptozotocin at 4 and 8 weeks[6] Dosage: 100 mg/kg/d Administration: i.g. 6 weeks Result: Improved pathological structures of neurites and myelin. Increased SOD, CAT and GPX protein levels in sciatic nerves. Decrease aldose reductase level in sciatic nerves. Clinical Trial

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研究领域：Metabolic Enzyme/Protease

作用靶点：Aldose Reductase

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参考文献：

[1]. Ramirez, M.A. and N.L. Borja, Epalrestat: an aldose reductase inhibitor for the treatment of diabetic neuropathy. Pharmacotherapy, 2008. 28(5): p. 646-55.

[2]. Okamoto, H., et al., Effects of epalrestat, an aldose reductase inhibitor, on diabetic neuropathy and gastroparesis. Intern Med, 2003. 42(8): p. 655-64.

[3]. Hotta, N., et al., Clinical investigation of epalrestat, an aldose reductase inhibitor, on diabetic neuropathy in Japan: multicenter study. Diabetic Neuropathy Study Group in Japan. J Diabetes Complications, 1996. 10(3): p. 168-72.

[4]. He J, et al. The aldose reductase inhibitor epalrestat exerts nephritic protection on diabetic nephropathy in db/db mice through metabolic modulation. Acta Pharmacol Sin. 2019 Jan;40(1):86-97.

[5]. Sato K, et al. Epalrestat increases intracellular glutathione levels in Schwann cells through transcription regulation. Redox Biol. 2013 Nov 19;2:15-21.

[6]. Li QR, et al. Epalrestat protects against diabetic peripheral neuropathy by alleviating oxidative stress and inhibiting polyol pathway. Neural Regen Res. 2016 Feb;11(2):345-51.

[7]. Zhang T, et al. The Aldose Reductase Inhibitor Epalrestat Maintains Blood-Brain Barrier Integrity by Enhancing Endothelial Cell Function during Cerebral Ischemia. Mol Neurobiol. 2023 Jul;60(7):3741-3757.