αIIbβ3 Antagonist

Echistatin is a naturally derived RGD-containing snake venom peptide. Echistatin exhibits an IC₅₀ of 0.6 nM against mouse α_vβ₃ integrin, and acts as an antagonist against α_vβ₃, α_IIbβ₃, α₅β₁ integrins, pp125^FAK and paxillin. Echistatin reduces the phosphorylation of pp125^FAK and paxillin, inhibits the autophosphorylation and kinase activity of pp125^FAK, and weakens its binding to pp60^src and paxillin. Echistatin disrupts the actin cytoskeleton and focal adhesions, induces melanoma cell detachment from fibronectin, and regulates cell adhesion and motility. Echistatin inhibits osteoclast maturation and migration, bone resorption, platelet aggregation, bone loss, as well as adhesion and metastasis of Lewis lung cancer cells; it also increases the number of osteoclasts and bone coverage area in mice with secondary hyperparathyroidism. Echistatin can be used in research related to melanoma, lung cancer and secondary hyperparathyroidism.

Echistatin TFA is a naturally derived RGD-containing snake venom peptide. Echistatin TFA exhibits an IC₅₀ of 0.6 nM against mouse α_vβ₃ integrin, and acts as an antagonist against α_vβ₃, α_IIbβ₃, α₅β₁ integrins, pp125^FAK and paxillin. Echistatin TFA reduces the phosphorylation of pp125^FAK and paxillin, inhibits the autophosphorylation and kinase activity of pp125^FAK, and weakens its binding to pp60^src and paxillin. Echistatin TFA disrupts the actin cytoskeleton and focal adhesions, induces melanoma cell detachment from fibronectin, and regulates cell adhesion and motility. Echistatin TFA inhibits osteoclast maturation and migration, bone resorption, platelet aggregation, bone loss, as well as adhesion and metastasis of Lewis lung cancer cells; it also increases the number of osteoclasts and bone coverage area in mice with secondary hyperparathyroidism. Echistatin TFA can be used in research related to melanoma, lung cancer and secondary hyperparathyroidism.

ME-3277 is a potent GPIIb/IIIa antagonist. ME-3277 reduces cerebral infarction without enhancing intracranial hemorrhage in photothrombotic occlusion of rabbit middle cerebral artery (MCA). ME-3277 can be used for the acute cerebral infarction research.