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BTT-3033

CAS No. : 1259028-99-3

MCE 国际站：BTT-3033

产品活性：BTT-3033 是一种具有口服活性的构象选择性的 α2β1 (EC50: 130 nM) 抑制剂，可与 α2I domain 结合。BTT-3033 抑制血小板与 collagen Ⅰ 结合和细胞增殖，并诱导细胞凋亡 (apoptosis)。BTT-3033 可用于前列腺癌、炎症和心血管疾病的研究。

研究领域：Cytoskeleton  |  Apoptosis

作用靶点：Integrin  |  Apoptosis

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.
BTT-3033 (10 μM, 5 min) inhibits human platelet binding to collagenⅠcoated capillaries under flow, with the EC₅₀ value for mouse whole blood to be 6 μM.
BTT-3033 (10 μM, 5 min) inhibits binding of α2-expressing CHO cells to collagen Ⅰ under shear stress conditions.
BTT-3033 (1 μM, 60 min) inhibits of neurogenic and thromboxane A2‐induced human prostate smooth muscle contraction.
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.
BTT-3033 (50 μM, 48 h) induces apoptosis through the activation of ROS, Bax protein upregulation, caspase‐3 activation, and depletion of ΔΨm.
BTT-3033 (10 μM, 15/28 days) suppresses MMP13 expression, increases the expression of MMP1 and MT-MMP1 in human articular cartilage‑derived chondrocytes.

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.
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.

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