产品
编 号：F099304
分子式：C23H20FN5O3S
分子量：465.5
分子式：C23H20FN5O3S
分子量：465.5
产品类型
规格
价格
是否有货
5mg
询价
询价
10mg
询价
询价
25mg
询价
询价
50mg
询价
询价
结构图
CAS No: 1259028-99-3
产品详情
生物活性：
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.
体内研究：
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 model
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)
Dosage:10 mg/kg for a single dose
Administration:Oral administration
Result:Plasma levels: about 1 ng/mL at 24 h post-dose.
体外研究：
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.
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.
体内研究：
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 model
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)
Dosage:10 mg/kg for a single dose
Administration:Oral administration
Result:Plasma levels: about 1 ng/mL at 24 h post-dose.
体外研究：
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.
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