Details
| Stereochemistry | RACEMIC |
| Molecular Formula | C15H16N4O2 |
| Molecular Weight | 284.3131 |
| Optical Activity | ( + / - ) |
| Defined Stereocenters | 0 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CC(CNC(=O)C1=CC=CN=C1)NC(=O)C2=CN=CC=C2
InChI
InChIKey=KTXBOOWDLPUROC-UHFFFAOYSA-N
InChI=1S/C15H16N4O2/c1-11(19-15(21)13-5-3-7-17-10-13)8-18-14(20)12-4-2-6-16-9-12/h2-7,9-11H,8H2,1H3,(H,18,20)(H,19,21)
| Molecular Formula | C15H16N4O2 |
| Molecular Weight | 284.3131 |
| Charge | 0 |
| Count |
|
| Stereochemistry | RACEMIC |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 1 |
| E/Z Centers | 0 |
| Optical Activity | ( + / - ) |
Nicaraven is a hydroxyl radical scavenger with antivasospastic and neuroprotective effects. Chugai (the Japanese subsidiary of Roche) is developing nicaraven (Antevas), a water-soluble antioxidant, for the potential treatment of disorders caused by acute cerebrovascular diseases. A registration application was filed in April 1995, and in April 2002, nicaraven was still awaiting registration in Japan. By August 2002, Chugai had filed an NDA in Japan for the additional indication of subarachnoidal bleeding.
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL3390820 Sources: https://www.ncbi.nlm.nih.gov/pubmed/17094462 |
1.5 mM [IC50] | ||
Target ID: WP408 Sources: https://www.ncbi.nlm.nih.gov/pubmed/12625035 |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | Unknown Approved UseUnknown |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Nicaraven, a Potential Radioprotective Agent, has Very Limited Effects on the Survival of Cancer Cells and the Growth of Established Tumors. | 2017-02-22 |
|
| The potential benefits of nicaraven to protect against radiation-induced injury in hematopoietic stem/progenitor cells with relative low dose exposures. | 2014-09-26 |
|
| Effects of a hydroxyl radical scavenger on delayed ischemic neurological deficits following aneurysmal subarachnoid hemorrhage: results of a multicenter, placebo-controlled double-blind trial. | 1996-05 |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/8622153
4 g nicaraven infused intravenously for 6-8 hours once a day
Route of Administration:
Intravenous
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/10047928
The antiplatelet activities in vitro of nicaraven were examined. The concentrations of nicaraven tested were 3.50 x 10(-5) mol/L, 1.75 x 10(-4) mol/L, 3.50 x 10(-4) mol/L, and 1.75 x 10(-3) mol/L, respectively. The maximum aggregation rate induced by adenosine diphosphate (ADP) was significantly inhibited by nicaraven at concentration ranges of 3.50 x 10(-4) mol/L or higher in the healthy volunteer platelets. The maximum aggregation rate induced by collagen was significantly inhibited by 1.75 x 10(-3) mol/L of nicaraven. Using platelets from patients with cerebral thrombosis, the maximum aggregation rate induced by ADP was significantly inhibited by 1.75 x 10(-3) mol/L of nicaraven. Furthermore, the maximum aggregation rate induced by collagen were significantly reduced by 1.75 x 10(-3) mol/L of nicaraven.
| Substance Class |
Chemical
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SUPERSEDED |
| Related Record | Type | Details | ||
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SALT/SOLVATE -> PARENT | |||
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ENANTIOMER -> RACEMATE | |||
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ENANTIOMER -> RACEMATE |
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ACTIVE MOIETY |