BTT-3033 is an orally active conformation-selective inhibitor of α2β1 ( EC50 : 130 nM) by binding to the α2I domain. BTT-3033 inhibits platelet binding to collagen Ⅰ and cell proliferation, and induces cell apoptosis . BTT-3033 can be used in the research of prostate cancer , inflammation and cardiovascular disease.