BTT-3033

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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。

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.

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 Ⅰunder 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.:Cell Viability AssayCell 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 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 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).

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.Animal Model:PAF (platelet-activating factor)-induced mouse air pouch modelDosage: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)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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Apoptosis

Apoptosis

Apoptosis | Integrin

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1259028-99-3

465.5

C23H20FN5O3S

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 250 mg/mL (537.06 mM; 超声助溶 )

CN(c1ccc(NC(=O)Nc2ccccc2)cc1)S(=O)(=O)c1cnn(c1)-c1ccc(F)cc1

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(-20℃)

With Ice Pack

≥ 2 years