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  1. Cytoskeleton
  2. Integrin
  3. Tirofiban

Tirofiban  (Synonyms: 替羅非班; L700462; MK383)

目錄號(hào): HY-17369B 純度: 99.88%
COA 產(chǎn)品使用指南

Tirofiban (L700462) 是一種選擇性和可逆性的血小板整合素受體 (Gp IIb/IIIa) 拮抗劑,能抑制纖維蛋白原與該受體結(jié)合,具有抗血栓活性。Tirofiban 可通過(guò)誘導(dǎo) VEGF 的產(chǎn)生來(lái)刺激內(nèi)皮細(xì)胞的遷移和增殖。Tirofiban 可通過(guò)緩解缺血區(qū)的心肌微血管結(jié)構(gòu)和內(nèi)皮功能障礙顯著減少心肌無(wú)回流和缺血再灌注損傷,從而改善心臟功能。

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Tirofiban Chemical Structure

Tirofiban Chemical Structure

CAS No. : 144494-65-5

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MCE 顧客使用本產(chǎn)品發(fā)表的 1 篇科研文獻(xiàn)

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

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]

體外研究
(In Vitro)

Tirofiban (0.25、1、3 μg/mL;72 小時(shí)) 增加 HAEC 細(xì)胞的增殖[1]。
Tirofiban (24 小時(shí)) 在 18 小時(shí)內(nèi)關(guān)閉 HUVEC 遷移的劃痕[1]。
Tirofiban (0.25,1 μg/mL;1小時(shí)) 在30分鐘后誘導(dǎo)產(chǎn)生VEGF,刺激內(nèi)皮細(xì)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.
體內(nèi)研究
(In Vivo)

Tirofiban (60 μg/kg;靜脈注射;一次) 顯示出通過(guò)增加 HR、LVESP、dp/dtmax 和降低 LVEDP 來(lái)增加收縮力、心室順應(yīng)性和改善心臟功能的活性[2]。
Tirofiban (60 μg/kg;靜脈注射;一次) 增強(qiáng) eNOS 活性,降低 iNOS 活性并減少 AMI 后再灌注后的無(wú)復(fù)流面積[2]。
Tirofiban (50 μg/per;irrigate;單劑量) 在擠壓模型中顯示出抗凝作用,微血管吻合后 24 小時(shí)通暢率為 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 號(hào)
性狀

固體

顏色

White to off-white

中文名稱(chēng)

替羅非班

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲(chǔ)存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn): 

1M HCl 中的溶解度 : 50 mg/mL (113.48 mM; 超聲助溶; 酸性條件溶解 (HCL 調(diào)節(jié),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)

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)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
查看完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用,-20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動(dòng)物溶解方案計(jì)算器
請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息:

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

由于實(shí)驗(yàn)過(guò)程有損耗,建議您多配一只動(dòng)物的量
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料
參考文獻(xiàn)

Tirofiban 相關(guān)分類(lèi)

完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效
儲(chǔ)備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用,-20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)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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產(chǎn)品名稱(chēng):
Tirofiban
目錄號(hào):
HY-17369B
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