1. Cytoskeleton Apoptosis
  2. Integrin Apoptosis
  3. BTT-3033

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。

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BTT-3033 Chemical Structure

BTT-3033 Chemical Structure

CAS No. : 1259028-99-3

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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[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 EC50 value 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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

Formula

C23H20FN5O3S

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 250 mg/mL (537.06 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.1482 mL 10.7411 mL 21.4823 mL
5 mM 0.4296 mL 2.1482 mL 4.2965 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 99.22%

参考文献

BTT-3033 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1482 mL 10.7411 mL 21.4823 mL 53.7057 mL
5 mM 0.4296 mL 2.1482 mL 4.2965 mL 10.7411 mL
10 mM 0.2148 mL 1.0741 mL 2.1482 mL 5.3706 mL
15 mM 0.1432 mL 0.7161 mL 1.4322 mL 3.5804 mL
20 mM 0.1074 mL 0.5371 mL 1.0741 mL 2.6853 mL
25 mM 0.0859 mL 0.4296 mL 0.8593 mL 2.1482 mL
30 mM 0.0716 mL 0.3580 mL 0.7161 mL 1.7902 mL
40 mM 0.0537 mL 0.2685 mL 0.5371 mL 1.3426 mL
50 mM 0.0430 mL 0.2148 mL 0.4296 mL 1.0741 mL
60 mM 0.0358 mL 0.1790 mL 0.3580 mL 0.8951 mL
80 mM 0.0269 mL 0.1343 mL 0.2685 mL 0.6713 mL
100 mM 0.0215 mL 0.1074 mL 0.2148 mL 0.5371 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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