Details
Stereochemistry | ACHIRAL |
Molecular Formula | C18H13N7 |
Molecular Weight | 327.3427 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
NC1=NNC2=NN=C(C=C12)C3=C4C=CC=CN4N=C3C5=CC=CC=C5
InChI
InChIKey=XVECMUKVOMUNLE-UHFFFAOYSA-N
InChI=1S/C18H13N7/c19-17-12-10-13(20-22-18(12)23-21-17)15-14-8-4-5-9-25(14)24-16(15)11-6-2-1-3-7-11/h1-10H,(H3,19,21,22,23)
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/16139248Curator's Comment: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/17123065 | https://www.ncbi.nlm.nih.gov/pubmed/24704674
Sources: https://www.ncbi.nlm.nih.gov/pubmed/16139248
Curator's Comment: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/17123065 | https://www.ncbi.nlm.nih.gov/pubmed/24704674
FR 180204 is a novel and selective inhibitor of extracellular signal-regulated kinase (ERK), which may be a potential new therapy for rheumatoid arthritis. FR 180204 inhibited ERK1 and ERK2 with an IC50 value of 0.51 uM (Ki = 0.31 uM) and 0.33 uM (Ki = 0.14 uM), respectively. FR 180204 may be useful as a therapeutic agent for the treatment of cancer, immune diseases, ischemic brain injury, and obesity. In a mouse model of dengue virus (DENV) infection, FR 180204 limits hepatocyte apoptosis, reduces DENV-induced liver injury, and improves Clinical parameters.
Originator
Sources: https://www.ncbi.nlm.nih.gov/pubmed/16139248
Curator's Comment: Ohori M et al., Lead Discovery Research Laboratories, Astellas Pharma Inc., Japan
Approval Year
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/17123065
Mice: In collagen-induced arthritis mice, FR 180204 (100 mg/kg, i.p., b.i.d.) significantly decreases the severity of symptoms and body weight loss.
Route of Administration:
Intraperitoneal
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/16139248
FR 180204 dose-dependently inhibited AP-1 transactivation,
with an IC50 of 3.1 uM.
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