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BTT 3033 是一种口服活性的 α2β1 (EC50: 130 nM) 构象选择性抑制剂,通过与 α2I 结构域结合。
Selective inhibitor of integrin α2β1 (EC50 = 130 nM for α2β1 binding to collagen I). Binds to the α2I domain. Exhibits selectivity for α2β1 over integrins α3β1, α4β1, α5β1 and αv. Inhibits platelet aggregation to collagen I coated capillaries under flow. Also inhibits binding of α2-expressing CHO cells to collagen I under shear stress conditions.
Nissinen et al (2012) Novel a2 beta 1 integrin inhibitors reveal that integrin binding to collagen under shear stress conditions does not require receptor preactivation. J.Cell Biol. 287 44694 PMID:23132859
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