中文名称
Tirofiban hydrochloride monohydrate
中文别名
盐酸替罗非班;N-(正丁基磺酰基)-O-[4-(4-***基)丁基]-L-酪氨酸盐酸盐水合物;盐酸替罗非班一水合物;替罗非班盐酸盐水合物;4-(4-吡啶基)-丁醇;消旋盐酸替罗非班;盐酸替罗非班单水合物;盐酸替罗非班一水;替罗非班;N-(丁基磺酰基)-O-[4-(4-***基)丁基]-L-酪氨酸盐酸盐 一水合物;替罗非班盐酸盐一水;盐酸替罗非班一水和物;盐酸替罗非班(标准品);替罗非班盐酸盐一水合物;N-丁磺酰基-(4-(4-吡啶基)丁基)-L-酪氨酸盐酸盐水合物;N-(正丁基磺酰基)-O-[4-(4-吡啶基)丁基]-L-酪氨酸盐酸盐水合物;盐酸替罗非班水合物
英文名称
Tirofiban hydrochloride monohydrate
英文别名
Tirofiban hydrochloride monohydrate;TIROFIBAN, HYDROCHLORIDE HYDRATE;Tirofiban HCl;N-(Butylsulfonyl)-O-[4-(4-piperidynyl)butyl]-L-tyrosine, Hydrochloride Hydrate;(2S)-2-(Butylsulfonylamino)-3-[4-[4-(4-piperidyl)butoxy]phenyl]propanoic acid hydrochloride hydrate;N-(Butylsulfonyl)-O-(4-(4-piperidinyl)butyl)-L-tyrosine monohydrochloride monohydrate;L-Tyrosine, N-(butylsulfonyl)-o-(4-(4-piperidinyl)butyl)-, monohydrochloride, monohydrate;Tirofiban Hydrochlor;Tirofiban Hydrochloride;(2S)-2-(butylsulfonylamino)-3-[4-(4-piperidin-4-ylbutoxy)phenyl]propanoic acid,hydrate,hydrochloride;L 700462 MK 383 N-(butylsulfonyl)-O-[4-(4-piperidinyl)butyl]-L-tyrosine;N-(Butylsulfonyl)-O-[4-(4-piperidinyl)butyl]-L-tyrosine Hydrochloride Monohydrate;Unii-6H925F8o5j;Tirofiban HCl Hydrate;Tirofiban hcl Monohydrate;4-(4-Pyridinyl)butanol hydrochloride
Cas No.
150915-40-5
分子式
C22H36N2O5S.HCl.H2O
分子量
495.07
包装储存
4°C, sealed storage, away from moisture
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
| 生物活性 | Tirofiban (L700462) hydrochloride monohydrate is a selective and reversible platelet integrin receptor (Gp IIb/IIIa) antagonist that inhibits fibrinogen binding to this receptor and has antithrombotic activity. Tirofiban hydrochloride monohydrate induces proliferation and migration on endothelial cell by inducing production of VEGF. 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. |
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| IC50 & Target[1][2] | |
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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.
Tirofiban hydrochloride monohydrate (24 hours) closes the scratch of HUVECs migration within 18 hours.
Tirofiban hydrochloride monohydrate (0.25, 1 μg/mL; 1 hour) induces production of VEGF after 30 minutes which can stimulates proliferation of endothelial cells. Medlife has not independently confirmed the accuracy of these methods. They are for reference only. Cell Proliferation Assay | Cell Line: | HAEC cells | | Concentration: | 0.25, 1, 3 μg/mL | | Incubation Time: | 72 hours | | Result: | Increased proliferation of HAEC cells. |
Cell Migration Assay | Cell Line: | HUVEC cells | | Concentration: | | | Incubation Time: | 24 hours | | Result: | Stimulated the migratory capacity of endothelial cells. |
Western Blot Analysis | 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.
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. 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. Medlife 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). | | 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) | | 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 or refrigerated transportation. |
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| 储存方式 | 4°C, sealed storage, away from moisture |
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| ClinicalTrial | |
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| 参考文献 | |
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引用地址：http://www.med-life.cn/
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