For research use only. Not for therapeutic Use.
Risarestat (CT-112), an aldose reductase inhibitor, is developed for the treatment of diabetic complications.
Risarestat inhibits the accumulation of dulcitol in a dose-dependent manner, except for the 1.0% solution which has an activity comparable to the 0.25% solution[1]. Risarestat peaks in the corneal epithelium, stroma, endothelium and aqueous humor in 30 minutes following instillation, then gradually diminishes time-dependently over a period of 24 hours. Risarestat remains detectable in the lens up to 24 hours, with a peak concentration at 2 hours after instillation[2]. The anterior surface area of superficial cells in the group treated with Risarestat is significantly decreases from a mean value of 881 to 728 microns2. Corneal sensitivity significantly improves from 5.36 to 1.37 g/mm2[3]. Animals treated with Risarestat shows a significant increase in the mean blinkresponse compared to untreated galactose-fed rats and does not differ significantly from controls towards the completion of the 7 month study. Animals treated topically with Risarestat and untreated galactose-fed rats develop bilateral nuclear cataracts within 3 weeks[4].
| Catalog Number | I013528 |
| CAS Number | 79714-31-1 |
| Synonyms | 5-(3-ethoxy-4-pentoxyphenyl)-1,3-thiazolidine-2,4-dione |
| Molecular Formula | C16H21NO4S |
| Purity | ≥95% |
| InChI | InChI=1S/C16H21NO4S/c1-3-5-6-9-21-12-8-7-11(10-13(12)20-4-2)14-15(18)17-16(19)22-14/h7-8,10,14H,3-6,9H2,1-2H3,(H,17,18,19) |
| InChIKey | CRPGRUONUFDYBG-UHFFFAOYSA-N |
| SMILES | CCCCCOC1=C(C=C(C=C1)C2C(=O)NC(=O)S2)OCC |
| Reference | [1]. Awata T, et al. Effect of an aldose reductase inhibitor, CT-112, on healing of the corneal epithelium in galactose-fed rats. J Ocul Pharmacol. 1988 Fall;4(3):195-201. [2]. Ohashi Y, et al. Intraocular penetration of CT-112, an aldose reductase inhibitor, following topical instillation. J Ocul Pharmacol. 1989 Winter;5(4):325-8. [3]. Hosotani H, et al. Reversal of abnormal corneal epithelial cell morphologic characteristics and reduced corneal sensitivity in diabetic patients by aldose reductase inhibitor, CT-112. Am J Ophthalmol. 1995 Mar;119(3):288-94. [4]. Jacot JL, et al. Diabetic-like corneal sensitivity loss in galactose-fed rats ameliorated with aldose reductase inhibitors. J Ocul Pharmacol Ther. 1998 Apr;14(2):169-80. |
