体外研究
(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 collagenⅠcoated capillaries under flow, with the EC50value 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].
Cell Viability Assay[4] | Cell Line: | LNcap‐FGC, and DU‐145 cells | | Concentration: | 0.05, 0.5 5, 25, and 50 μM | | Incubation Time: | 48 h | | Result: | Decreased the cell viability at 25 μM and 50 μM. |
Cell Viability Assay[4] | Cell Line: | LNcap‐FGC, and DU‐145 cells | | Concentration: | 5, 25, and 50 μM | | Incubation Time: | 48 h | | Result: | Induced cell apoptosis about 20%, 32%, and 47% (LNcap‐FGC) and 26%, 41%, and 59% (DU‐145) at 5, 25, and 50 μM. |
Western Blot Analysis[4] | Cell Line: | LNcap‐FGC, and DU‐145 cells | | Concentration: | 25 μM | | Incubation Time: | 48 h | | Result: | Resulted in down-regulation of N‐cadherin and upregulation of E‐cadherin (EMT‐associated proteins). |
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体内研究
(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].
| Animal Model: | PAF (platelet-activating factor)-induced mouse air pouch model[2] | | Dosage: | 1, 10 mg/kg at 24 h and 2 h before PAF induction | | Administration: | Oral administration | | Result: | Reduced the infiltration of leukocytes by about 50% at 10 mg/kg. |
| Animal Model: | Male DBA/1 mice (Pharmacokinetic assay)[2] | | Dosage: | 10 mg/kg for a single dose | | Administration: | Oral administration | | Result: | Plasma levels: about 1 ng/mL at 24 h post-dose. |
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