
MedChemExpress - Model Epalrestat - 82159-09-9
Epalrestat is an orally active aldose reductase inhibitor that acts on diabetic neuropathy[1][2][3].MCE products for research use only. We do not sell to patients.
Epalrestat
MCE China:Epalrestat
Brand:MedChemExpress (MCE)
Cat. No.HY-66009
CAS:82159-09-9
Synonyms:ONO2235
Purity:99.72%
Storage:-20°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Shipping:Room temperature in continental US; may vary elsewhere.
Description:Epalrestat is an orally active aldose reductase inhibitor that acts on diabetic neuropathy.
In Vitro:Epalrestat (100 and 200 µM, 24 h) inhibits cell viability and induces cell apoptosis in rat Schwann cells (SCs)[5]. Epalrestat (10 and 50 µM, 24 h) increases intracellular glutathione levels in rat SCs by up-regulating γ-GCS via Nrf2 activation[5]. Epalrestat (50 µM, 16 h) protects SCs from oxidative stress[5].
In Vivo:Epalrestat (0.08% (w/w) in regular chow, 8 weeks) shows nephritic protective effect in diabetic nephropathy in db/db mice[4]. Epalrestat (100 mg/kg, i.g., daily for 6 weeks) protects rats from diabetic peripheral nerve injury in diabetic peripheral neuropathy (DPN) model induced by Streptozotocin (HY-13753)[6]. Epalrestat (50 mg/kg, oral gavage, twice a day) reduces cerebral ischemia-induced infarct volume and BBB permeability in mice[7].
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References:
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[5]. Sato K, et al. Epalrestat increases intracellular glutathione levels in Schwann cells through transcription regulation. Redox Biol. 2013 Nov 19;2:15-21. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
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