Israpafant is a highly selective and long-acting antagonist of the platelet activating factor (PAF) receptor, demonstrating potent inhibitory effects with IC50 values of 0.84 nM and 3.84 nM against PAF-induced aggregation in human and rabbit platelets, respectively. This compound has been shown to enhance both extracellular calcium influx and intracellular calcium release in prostate cancer cells. Additionally, Israpafant effectively attenuates allergic cutaneous responses, including eosinophilia, cytokine production, edema, and erythema, in murine models. These properties position Israpafant as a valuable tool for investigating PAF-related pathways and allergic reactions.
Israpafant is a highly selective and long-acting antagonist of the platelet activating factor (PAF) receptor, demonstrating potent inhibitory effects with IC50 values of 0.84 nM and 3.84 nM against PAF-induced aggregation in human and rabbit platelets, respectively. This compound has been shown to enhance both extracellular calcium influx and intracellular calcium release in prostate cancer cells. Additionally, Israpafant effectively attenuates allergic cutaneous responses, including eosinophilia, cytokine production, edema, and erythema, in murine models. These properties position Israpafant as a valuable tool for investigating PAF-related pathways and allergic reactions.
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