RISARESTAT

Details

Stereochemistry	RACEMIC
Molecular Formula	C16H21NO4S
Molecular Weight	323.407
Optical Activity	( + / - )
Defined Stereocenters	0 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CCCCCOC1=CC=C(C=C1OCC)C2SC(=O)NC2=O

InChI

InChIKey=CRPGRUONUFDYBG-UHFFFAOYSA-N

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)

HIDE SMILES / InChI

Molecular Formula	C16H21NO4S
Molecular Weight	323.407
Charge	0
Count

Stereochemistry	RACEMIC
Additional Stereochemistry	No
Defined Stereocenters	0 / 1
E/Z Centers	0
Optical Activity	( + / - )

Description
Sources: http://www.ncbi.nlm.nih.gov/pmc/articles/PMC1772556/pdf/bjo08900266.pdf
Curator's Comment: Description was created based on several sources, including http://www.ncbi.nlm.nih.gov/pubmed/8562538

RISARESTAT is an aldose reductase inhibitor. It has been shown that topically applied RISARESTAT (CT-112) can penetrate the cornea at sufficient concentrations to inhibit the activity of AR in the lens and can be taken up by the endothelial cells. CT-112 was shown to improve the corneal epithelial barrier function in diabetic patients.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Aldose reductase 44 Target ID: CHEMBL1900 Sources: https://www.jstage.jst.go.jp/article/cpb1958/30/10/30_10_3601/_pdf	Inhibitor 8297

Conditions

Condition	Modality	Targets	Highest Phase	Product
Diabetes mellitus 91 Sources: http://www.ncbi.nlm.nih.gov/pmc/articles/PMC505343/pdf/brjopthal00024-0012.pdf	Primary		Withdrawn	Unknown Approved Use Unknown

PubMed

Title	Date	PubMed
Topical aldose reductase inhibitor for correcting corneal endothelial changes in diabetic patients.	1995 Dec	8562538
A randomised, placebo controlled clinical trial of the aldose reductase inhibitor CT-112 as management of corneal epithelial disorders in diabetic patients.	2005 Mar	15722300

Patents

Sample Use Guides

In Vivo Use Guide

0.25% eye drops of RISARESTAT (CT-112) four times a day for 8 weeks.

Route of Administration: Topical

In Vitro Use Guide

50% inhibition-concentration in the medium was 3.78-5.92 x 10(-7) M for RISARESTAT (CT-112), and the resulting concentration of drug in the lens was 21.19-24.63 nmole/g lens for CT-112.

Substance Class	Chemical Created by `admin` on `Fri Dec 15 16:25:19 GMT 2023` Edited by `admin` on `Fri Dec 15 16:25:19 GMT 2023`
Record UNII	6I9DQB98QI
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

RISARESTAT

Official Name

English

RISRESTAT

Common Name

English

CT-112

Code

English

2,4-THIAZOLIDINEDIONE, 5-(3-ETHOXY-4-(PENTYLOXY)PHENYL)-

Systematic Name

English

(±)-5-(3-ETHOXY-4-(PENTYLOXY)PHENYL)-2,4-THIAZOLIDINEDIONE

Systematic Name

English

risarestat [INN]

Common Name

English

RISRESTAT [JAN]

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C471