951015-69-3
Chemical Structure
EVT-401
- CAS No.: 951015-69-3
- Formula:C22H20F4N2O3
- Molecular Weight:436.40
InChIKey: JECILOFRRYCNDH-CYBMUJFWSA-N
SMILES: FC(C=C1CC(NC2=C3C(C(N(C=C3)[C@H](C)CO)=O)=CC=C2C)=O)=C(C=C1)C(F)(F)F
Biological Activity: EVT-401 is an orally active, potent and highly selective human P2X7R antagonist, with an IC50 of 10 nM and a Ki of 7.6 nM for human P2X7R, and an IC50 of 220 nM for mouse P2X7R. EVT-401 promotes apoptosis and induces cell cycle arrest in human rheumatoid arthritis synovial fibroblasts (RA SF), reduces the production of proinflammatory and joint-destructive mediators, and mitigates aggressive phenotypes. EVT-401 exhibits favorable oral bioavailability and a good safety profile, making it suitable for research into rheumatoid arthritis[1].
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EVT-401 | EVT-401 is an orally active, potent and highly selective human P2X7R antagonist, with an IC50 of 10 nM and a Ki of 7.6 nM for human P2X7R, and an IC50 of 220 nM for mouse P2X7R. EVT-401 promotes apoptosis and induces cell cycle arrest in human rheumatoid arthritis synovial fibroblasts (RA SF), reduces the production of proinflammatory and joint-destructive mediators, and mitigates aggressive phenotypes. EVT-401 exhibits favorable oral bioavailability and a good safety profile, making it suitable for research into rheumatoid arthritis. | |||||||||||||||||||||
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Keywords
