Formulation: A solid
Formal Name: 2-(5,6-diethoxy-7-fluoro-1,3-dihydro-1-imino-2H-isoindol-2-yl)-1-[3-(1,1-dimethylethyl)-4-methoxy-5-(4-morpholinyl)phenyl]-ethanone, monohydrobromide
Purity: ≥95%
Formula Markup: C29H38FN3O5 • HBr
Formula Weight: 608,5
Shelf life (days): 1460
CAS Number: 474550-69-1
Notes: Atopaxar is an antagonist of proteinase-activated receptor 1 (PAR1; IC50 = 0.019 µM).{69957} It selectively inhibits thrombin- or TRAP-6 amide-induced aggregation of isolated human platelet-rich plasma (IC50s = 0.064 and 0.09 µM, respectively) over ADP-, PAR4-AP-, U-46619-, or collagen-induced aggregation of isolated human platelet-rich plasma at 10 µM. Atopaxar (10 µM) inhibits IL-6-induced phosphorylation of STAT3 in A549 non-small cell lung cancer (NSCLC) cells and transactivation of STAT3 in a reporter assay using A549 cells (IC50 = 5.901 µM).{69958} It reduces granzyme B- and IL-1β-induced cytotoxicity in human neurons derived from induced pluripotent stem cells (iPSCs) when used at a concentration of 1 µM.{69959} Atopaxar (30 and 100 mg/kg) increases the time to occlusion of the femoral artery but does not affect bleeding time in a guinea pig model of photochemically induced thrombosis.{69957}
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