U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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 of RISARESTAT

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

Description
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

Curator's Comment: A European patent application was jointly filed by the Japanese companies Takeda and Senju and published in August 1981 http://worldwide.espacenet.com/publicationDetails/biblio?CC=EP&NR=0033617A2&KC=A2&FT=D # Takeda Chemical Industries, Ltd. and Senju Pharmaceutical Co.,Ltd.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Unknown

Approved Use

Unknown
PubMed

PubMed

TitleDatePubMed
Patents

Sample Use Guides

0.25% eye drops of RISARESTAT (CT-112) four times a day for 8 weeks.
Route of Administration: Topical
In Vitro Use Guide
Curator's Comment: Rat lenses were cultured in a medium containing either 30mM xylose or 30mM glucose. Inhibitory effect of RISARESTAT (CT-112), on the accumulation of sugar alcohols and the concentration of the drug in the lens was measured.
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.
Name Type Language
RISARESTAT
INN  
INN  
Official Name English
RISRESTAT
JAN  
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
Created by admin on Fri Dec 15 16:25:19 GMT 2023 , Edited by admin on Fri Dec 15 16:25:19 GMT 2023
Code System Code Type Description
MESH
C051003
Created by admin on Fri Dec 15 16:25:19 GMT 2023 , Edited by admin on Fri Dec 15 16:25:19 GMT 2023
PRIMARY
CAS
79714-31-1
Created by admin on Fri Dec 15 16:25:19 GMT 2023 , Edited by admin on Fri Dec 15 16:25:19 GMT 2023
PRIMARY
PUBCHEM
133264
Created by admin on Fri Dec 15 16:25:19 GMT 2023 , Edited by admin on Fri Dec 15 16:25:19 GMT 2023
PRIMARY
EPA CompTox
DTXSID7048796
Created by admin on Fri Dec 15 16:25:19 GMT 2023 , Edited by admin on Fri Dec 15 16:25:19 GMT 2023
PRIMARY
ChEMBL
CHEMBL1983865
Created by admin on Fri Dec 15 16:25:19 GMT 2023 , Edited by admin on Fri Dec 15 16:25:19 GMT 2023
PRIMARY
FDA UNII
6I9DQB98QI
Created by admin on Fri Dec 15 16:25:19 GMT 2023 , Edited by admin on Fri Dec 15 16:25:19 GMT 2023
PRIMARY
INN
7936
Created by admin on Fri Dec 15 16:25:19 GMT 2023 , Edited by admin on Fri Dec 15 16:25:19 GMT 2023
PRIMARY
NCI_THESAURUS
C90847
Created by admin on Fri Dec 15 16:25:19 GMT 2023 , Edited by admin on Fri Dec 15 16:25:19 GMT 2023
PRIMARY
SMS_ID
300000034384
Created by admin on Fri Dec 15 16:25:19 GMT 2023 , Edited by admin on Fri Dec 15 16:25:19 GMT 2023
PRIMARY