Tirofiban (L700462) hydrochloride monohydrate 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 hydrochloride monohydrate 可通过诱导 VEGF 的产生来刺激内皮细胞的迁移和增殖。Tirofiban hydrochloride monohydrate 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。
| 生物活性 | Tirofiban (L700462) hydrochloride monohydrate is a selective and reversible plateletintegrinreceptor (Gp IIb/IIIa) antagonist that inhibitsfibrinogenbinding to this receptor and has antithrombotic activity. Tirofiban hydrochloride monohydrate induces proliferation and migration on endothelial cell by inducing production ofVEGF. Tirofiban hydrochloride monohydrate 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]. |
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体外研究
(In Vitro) | Tirofiban hydrochloride monohydrate (0.25, 1, 3 μg/mL; 72 hours) increases proliferation of HAEC cells[1].
Tirofiban hydrochloride monohydrate (24 hours) closes the scratch of HUVECs migration within 18 hours[1].
Tirofiban hydrochloride monohydrate (0.25, 1 μg/mL; 1 hour) induces production of VEGF after 30 minutes which can stimulates proliferation of endothelial cells[1].
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. |
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体内研究
(In Vivo) | Tirofiban hydrochloride monohydrate (60 μg/kg; i.v.; once) shows activity of increasing contraction force, ventricular compliance, and improving heart function by increasing HR, LVESP, dp/dtmax, and reducing LVEDP[2].
Tirofiban hydrochloride monohydrate (60 μg/kg; i.v.; once) enhances eNOS activity, decreases iNOS activity and reduces area of no-reflow after reperfusion following AMI[2].
Tirofiban hydrochloride monohydrate (50 μg/per; irrigate; once) shows anticoagulant effect with patency rates of 59% at 24 hours after microvascular anastomosis in the crush model[3].
| 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%. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 溶解性数据 | In Vitro: DMSO : 100 mg/mL(201.99 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.0199 mL | 10.0996 mL | 20.1992 mL | | 5 mM | 0.4040 mL | 2.0199 mL | 4.0398 mL | | 10 mM | 0.2020 mL | 1.0100 mL | 2.0199 mL |
*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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: 2.5 mg/mL (5.05 mM); Suspended solution; Need ultrasonic
此方案可获得 2.5 mg/mL (5.05 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (5.05 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.05 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (5.05 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.05 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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