BTT-3033

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^[1][2][4]. In Vitro:BTT-3033 (1 nM-100 μM, 2 h) inhibits CHO-α2wt cell adhesion to rat tail collagen I (EC₅₀: 130 nM), exhibits selectivity for α2β1 over α3β1, α4β1, α5β1 and αv^[1].
BTT-3033 (10 μM, 5 min) inhibits human platelet binding to collagen I coated capillaries under flow, with the EC₅₀ value for mouse whole blood to be 6 μM^[1].
BTT-3033 (10 μM, 5 min) inhibits binding of α2-expressing CHO cells to collagen I under shear stress conditions^[1].
BTT-3033 (1 μM, 60 min) inhibits of neurogenic and thromboxane A2-induced human prostate smooth muscle contraction^[3].
BTT-3033 (25 and 50 μM, 48 h) inhibits cell viability and proliferation by inducing G1 cell cycle arrest in LNcap-FGC, and DU-145 cells^[4].
BTT-3033 (50 μM, 48 h) induces apoptosis through the activation of ROS, Bax protein upregulation, caspase-3 activation, and depletion of ΔΨm^[4].
BTT-3033 (10 μM, 15/28 days) suppresses MMP13 expression, increases the expression of MMP1 and MT-MMP1 in human articular cartilage derived chondrocytes^[5]. In Vivo:BTT-3033 (oral administration, 10 mg/kg, at 24 h and 2 h before PAF induction) shows anti-inflammatory effects in mouse air pouch model^[2].
BTT-3033 (oral administration, 10 mg/kg, at 48 ,24 and 2 h before ear swelling) shows anti-inflammatory effects in arachidonic acid-induced ear edema model^[2].