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BTT-3033
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
BTT-3033图片
CAS NO:1259028-99-3
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议

产品介绍
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。
生物活性

BTT-3033 is an orally active conformation-selective inhibitor ofα2β1(EC50: 130 nM) by binding to the α2I domain. BTT-3033 inhibits platelet binding to collagen Ⅰ and cell proliferation, and induces cellapoptosis. BTT-3033 can be used in the research of prostatecancer, inflammation andcardiovascular disease[1][2][4].

IC50& Target[1][5]

α2β1

130 nM (EC50)

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).
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.
分子量

465.50

性状

Solid

Formula

C23H20FN5O3S

CAS 号

1259028-99-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
In solvent-80°C6 months
-20°C1 month