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ChemicalBook--->CAS DataBase List--->79714-31-1

79714-31-1

79714-31-1 Structure

79714-31-1 Structure
IdentificationBack Directory
[Name]

CT 112
[CAS]

79714-31-1
[Synonyms]

Risarestat
RISARESTAT (CT-112)
CT 112 (reductase inhibitor)
5-(3-Ethoxy-4-pentoxyphenyl)thiazolidine-2,4-dione
5-(3-Ethoxy-4-pentyloxyphenyl)-2,4-thiazolidinedione
5-[3-Ethoxy-4-(pentyloxy)phenyl]-2,4-thiazolidinedione
2,4-Thiazolidinedione, 5-[3-ethoxy-4-(pentyloxy)phenyl]-
[Molecular Formula]

C16H21NO4S
[MDL Number]

MFCD01940023
[MOL File]

79714-31-1.mol
[Molecular Weight]

323.41
Chemical PropertiesBack Directory
[Boiling point ]

485.9±45.0 °C(Predicted)
[density ]

1.189±0.06 g/cm3(Predicted)
[form ]

Solid
[pka]

5.91±0.50(Predicted)
[color ]

White to light yellow
Hazard InformationBack Directory
[Uses]

Risarestat (CT-112), an aldose reductase inhibitor, is developed for the treatment of diabetic complications.
[Definition]

ChEBI: Risarestat is a thiazolidinone.
[in vivo]

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].

[References]

[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. DOI:10.1089/jop.1988.4.195
[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. DOI:10.1089/jop.1989.5.325
[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. DOI:10.1016/s0002-9394(14)71169-9
[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. DOI:10.1089/jop.1998.14.169
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