Epalrestat

SKU: orb1223938

Description

A noncompetitive and reversible aldose reductase inhibitor with IC50 of 10 nM and 26 nM for purified aldose reductase from rat lens and human placenta, respectively; used for the treatment of diabetic neuropathy.Diabetes Approved.

Key Properties

• CAS Number: 82159-09-9
• MW: 319.3986
• Purity: >98% (HPLC)
• Formula: C₁₅H₁₃NO₃S₂
• SMILES: O=C(O)CN(C/1=O)C(SC1=C/C(C)=C/C2=CC=CC=C2)=S
• Target: Aldose Reductase
• Solubility: DMSO: ≥ 3.1 mg/mL

Bioactivity

• In Vivo:
  Animal model: db/db mice. 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. 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.
• In Vitro:
  RT-PCR Cell line: rat SCs. Concentration: 10 or 50 μM. Incubation time: 4 h. Result: Increased the nuclear level of active Nrf2 by 1.8- and 3.8-fold at 10 and 50 μM, and failed to increase Nrf2 mRNA levels.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

ONO-2235

Quick Database Links

Gene Symbol

Aldose Reductase