ML-221

ML-221

CAT N°: 27313
Price:

97.00 82.45

ML-221 is an antagonist of the G protein-coupled receptor (GPCR) APJ (IC50 = 4.8 ?M).{48358} It is selective for APJ over the angiotensin II type 1 (AT1) receptor (IC50 = >78 ?M). ML-221 antagonizes apelin 13-induced activation of APJ in cAMP and ?-arrestin recruitment assays (IC50s = 0.7 and 1.75 ?M, respectively). It inhibits proliferation and angiogenesis in Mz-ChA-1 cholangiocarcinoma cells when used at concentrations ranging from 5 to 15 ?M.{48359} In vivo, ML-221 (150 ?g/kg) reduces tumor growth in a Mz-ChA-1 mouse xenograft model. Intrathecal injection of ML-221 (10 ?g per animal) reduces mechanical allodynia and heat hyperalgesia induced by chronic constriction injury (CCI) of the sciatic nerve in rats.{48360} ML-221 also inhibits pathological angiogenesis and enhances normal vessel recovery in retinal ischemic regions in a mouse model of oxygen-induced retinopathy.{48361}

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