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Tirofiban  (Synonyms: 替罗非班; L700462; MK383)

目录号: HY-17369B 纯度: 99.88%
COA 产品使用指南

Tirofiban (L700462) 是一种选择性和可逆性的血小板整合素受体 (Gp IIb/IIIa) 拮抗剂,能抑制纤维蛋白原与该受体结合,具有抗血栓活性。Tirofiban 可通过诱导 VEGF 的产生来刺激内皮细胞的迁移和增殖。Tirofiban 可通过缓解缺血区的心肌微血管结构和内皮功能障碍显著减少心肌无回流和缺血再灌注损伤,从而改善心脏功能。

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Tirofiban Chemical Structure

Tirofiban Chemical Structure

CAS No. : 144494-65-5

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MCE 顾客使用本产品发表的 1 篇科研文献

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Tirofiban (L700462) is a selective and reversible platelet integrin receptor (Gp IIb/IIIa) antagonist that inhibits fibrinogen binding to this receptor and has antithrombotic activity. Tirofiban induces proliferation and migration on endothelial cell by inducing production of VEGF. Tirofiban can significantly reduces myocardial no-reflow and ischemia-reperfusion injury by alleviating myocardial microvascular structural and endothelial dysfunction in the ischemic area[1][2][3].

IC50 & Target

Gp IIb/IIIa Receptor[1]

体外研究
(In Vitro)

Tirofiban (0.25、1、3 μg/mL;72 小时) 增加 HAEC 细胞的增殖[1]
Tirofiban (24 小时) 在 18 小时内关闭 HUVEC 迁移的划痕[1]
Tirofiban (0.25,1 μg/mL;1小时) 在30分钟后诱导产生VEGF,刺激内皮细胞增殖[1]

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

Cell Proliferation Assay[1]

Cell Line: HAEC cells
Concentration: 0.25, 1, 3 μg/mL
Incubation Time: 72 hours
Result: Increased proliferation of HAEC cells.

Cell Migration Assay [1]

Cell Line: HUVEC cells
Concentration:
Incubation Time: 24 hours
Result: Stimulated the migratory capacity of endothelial cells.

Western Blot Analysis[1]

Cell Line: HAEC cells
Concentration: 0.05, 0.12, 0.25, 1 μg/mL
Incubation Time: 1 hour
Result: Induced production of VEGF which stimulated proliferation of endothelial cells.
体内研究
(In Vivo)

Tirofiban (60 μg/kg;静脉注射;一次) 显示出通过增加 HR、LVESP、dp/dtmax 和降低 LVEDP 来增加收缩力、心室顺应性和改善心脏功能的活性[2]
Tirofiban (60 μg/kg;静脉注射;一次) 增强 eNOS 活性,降低 iNOS 活性并减少 AMI 后再灌注后的无复流面积[2]
Tirofiban (50 μg/per;irrigate;单剂量) 在挤压模型中显示出抗凝作用,微血管吻合后 24 小时通畅率为 59%[3]

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

Animal Model: Male Sprague-Dawley rats (10 to 15-week-age; 270-330 g)[2].
Dosage: 60 μg/kg
Administration: Intravenous injection; once.
Result: Increased contraction force, ventricular compliance, and improved heart function.
Reduced the size of no-reflow and infarct.
Animal Model: Sprague-Dawley rats (350-400 g; crush injury model)[3]
Dosage: 50 µg/per (50 µg/mL, 1 mL for each)
Administration: Irrigate 1 mL within the vessel lumen (before placement of the last suture); once.
Result: Showed anticoagulant effect with patency rates of 59%.
Clinical Trial
分子量

440.60

Formula

C22H36N2O5S

CAS 号
性状

固体

颜色

White to off-white

中文名称

替罗非班

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

1M HCl 中的溶解度 : 50 mg/mL (113.48 mM; 超声助溶; 酸性条件溶解 (HCL 调节,pH≈1))

H2O 中的溶解度 : < 0.1 mg/mL (insoluble)

DMSO 中的溶解度 : < 1 mg/mL (insoluble or slightly soluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2696 mL 11.3482 mL 22.6963 mL
5 mM 0.4539 mL 2.2696 mL 4.5393 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
参考文献

Tirofiban 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
1M HCl 1 mM 2.2696 mL 11.3482 mL 22.6963 mL 56.7408 mL
5 mM 0.4539 mL 2.2696 mL 4.5393 mL 11.3482 mL
10 mM 0.2270 mL 1.1348 mL 2.2696 mL 5.6741 mL
15 mM 0.1513 mL 0.7565 mL 1.5131 mL 3.7827 mL
20 mM 0.1135 mL 0.5674 mL 1.1348 mL 2.8370 mL
25 mM 0.0908 mL 0.4539 mL 0.9079 mL 2.2696 mL
30 mM 0.0757 mL 0.3783 mL 0.7565 mL 1.8914 mL
40 mM 0.0567 mL 0.2837 mL 0.5674 mL 1.4185 mL
50 mM 0.0454 mL 0.2270 mL 0.4539 mL 1.1348 mL
60 mM 0.0378 mL 0.1891 mL 0.3783 mL 0.9457 mL
80 mM 0.0284 mL 0.1419 mL 0.2837 mL 0.7093 mL
100 mM 0.0227 mL 0.1135 mL 0.2270 mL 0.5674 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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产品名称:
Tirofiban
目录号:
HY-17369B
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