ML221 is capable of suppressing the cultured-endothelial cell proliferation. In oxygen-induced retinopathy (OIR) mice model, ML221 can block the pathological angiogenesis and increase the recovery of normal vessels into the ischemic regions in the retina. It can also inhibit the formation of neovascular tufts.
ML221 is an antagonist of the apelin receptor (also known as APJ). ML221 blocks Apelin-13 mediated receptor activation (recruitment of β-arrestin) with an IC50 of 1.75 µM.
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