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Tirofiban hydrochloride monohydrate

糖蛋白IIb/IIIa抑制剂，Tirofiban盐酸盐一水合物是非肽类，糖蛋白IIb/IIIa拮抗剂。

目录号: PC14802 纯度: ≥98%

CAS No. :150915-40-5

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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-哌啶基)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-哌啶基)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.

性状

Solid

IC50 & Target[1][2]

Gp IIb/IIIa Receptor

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.

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%.

运输条件

Room temperature or refrigerated transportation.

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)

ClinicalTrial

参考文献

[1]. Giordano A, et al. Tirofiban induces VEGF production and stimulates migration and proliferation of endothelial cells. Vascul Pharmacol. 2014 May-Jun;61(2-3):63-71. [Information]

[2]. Liu X, et al. Effects of tirofiban on the reperfusion-related no-reflow in rats with acute myocardial infarction. J Geriatr Cardiol. 2013 Mar;10(1):52-8. [Information]

[3]. Yates YJ, et al. The effect of tirofiban on microvascular thrombosis: crush model. Plast Reconstr Surg. 2005 Jul;116(1):205-8 [Information]

溶解度数据

体外研究:

DMSO : 100 mg/mL (201.99 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

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

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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 (sealed storage, away from moisture)。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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.

建议依照次序添加每种溶剂： 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。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
2.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in 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 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

建议依照次序添加每种溶剂： 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。

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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