Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C17H11BrFN3O4 |
Molecular Weight | 420.189 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
FC1=C(CN2C(=O)C3=CC=CN3[C@@]4(CC(=O)NC4=O)C2=O)C=CC(Br)=C1
InChI
InChIKey=QCVNMNYRNIMDKV-QGZVFWFLSA-N
InChI=1S/C17H11BrFN3O4/c18-10-4-3-9(11(19)6-10)8-21-14(24)12-2-1-5-22(12)17(16(21)26)7-13(23)20-15(17)25/h1-6H,7-8H2,(H,20,23,25)/t17-/m1/s1
DescriptionSources: http://adisinsight.springer.com/drugs/800005030Curator's Comment: Description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/9767647 | https://www.ncbi.nlm.nih.gov/pubmed/24785785
Sources: http://adisinsight.springer.com/drugs/800005030
Curator's Comment: Description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/9767647 | https://www.ncbi.nlm.nih.gov/pubmed/24785785
Ranirestat (AS-3201, SX-3030, SX-3202) is an oral aldose reductase inhibitor. (-)-enantiomer (AS-3201) is 10 times more potent in inhibition of the aldose reductase and 500 times more potent in the in vivo activity than the corresponding (+)-enantiomer (SX-3202). Ranirestat is being developed by Dainippon Sumitomo Pharma (formerly Dainippon Pharmaceutical) for the treatment of diabetic complications, primarily diabetic neuropathy. Ranirestat is a well-tolerated front-line inhibitor. It reproducibly exhibits some degree of measurable objective beneficial outcomes in diabetic neuropathy.
CNS Activity
Sources: https://www.ncbi.nlm.nih.gov/pubmed/26384019
Curator's Comment: ranirestat showed minimal amount of CNS activity (limitation: simulation study)
Originator
Approval Year
Cmax
Value | Dose | Co-administered | Analyte | Population |
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3213 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/32437025 |
40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered: |
RANIRESTAT plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
3016 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/32437025 |
40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered: |
RANIRESTAT plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
3644 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/32437025 |
40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered: |
RANIRESTAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
60.4 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/32437025 |
40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered: |
RANIRESTAT plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
67 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/32437025 |
40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered: |
RANIRESTAT plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
71.1 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/32437025 |
40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered: |
RANIRESTAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
105.6 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/32437025 |
40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered: |
RANIRESTAT plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
131.6 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/32437025 |
40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered: |
RANIRESTAT plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
133.7 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/32437025 |
40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered: |
RANIRESTAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
Funbound
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
0.665% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/32437025 |
40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered: |
RANIRESTAT plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
1.03% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/32437025 |
40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered: |
RANIRESTAT plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
0.77% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/32437025 |
40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered: |
RANIRESTAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
Sample Use Guides
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/27190083
High glucose significantly increased sorbitol levels, superoxide generation and vascular cell adhesion molecule-1 mRNA levels in, and THP-1 cell adhesion to, human umbilical vein endothelial cells, all of which were prevented by 500 nM ranirestat
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Classification Tree | Code System | Code | ||
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NCI_THESAURUS |
C72880
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CHEMBL132846
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DTXSID80163642
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153948
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RANIRESTAT
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SUB32892
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C96307
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DB05327
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ACTIVE MOIETY