AZD2716 is an orally active secretory phospholipase A 2 ( sPLA 2 ) inhibitor. AZD2716 inhibits human GIIA sPLA 2 ( IC 50 =10 nM), human GV sPLA 2 ( IC 50 =40 nM), human GX sPLA 2 ( IC 50 =400 nM), snake venom sPLA 2 ( IC 50 =2 pM), and snake ( Bothrops jararacussu ) Lys49-PLA2-like toxin ( K d =110 μM). AZD2716 inhibits sPLA 2 isoforms IIa, V, X, snake venom sPLA 2 s, and snake venom Lys49-PLA 2 -like toxin myotoxic activity via hydrophobic channel binding. AZD2716 suppresses GIIA sPLA 2 production, neutralizes snake venom-induced myotoxicity, and improves survival in envenomed mice. AZD2716 can be used for the research of coronary artery disease, atherosclerosis, and snakebite envenoming.
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