Tirofiban hydrochloride monohydrate
Based on 6 publication(s) in Google Scholar
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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- Reinheit : 99.92%
- CAS. Nr.: 150915-40-5
- Formel: C22H39ClN2O6S
- Molecular Weight:495.07
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Speicherung:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
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TR-14035α4β7/α4β1 Antagonist
Publications Citing Use of MedChemExpress (MCE) Tirofiban hydrochloride monohydrate
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Customer Validation & Images
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Bio/Physico-chemical Assay
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Cell Proliferation/Viability Assay
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Cell Migration/Invasion Assay
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ELISA
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ELISA
Biologische Aktivität
Beschreibung
IC50 & Target
Gp IIb/IIIa Receptor[1]
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:HAEC cells
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Concentration:0.25, 1, 3 μg/mL
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Incubation Time:72 hours
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Result:Increased proliferation of HAEC cells.
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Cell Line:HUVEC cells
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Concentration:
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Incubation Time:24 hours
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Result:Stimulated the migratory capacity of endothelial cells.
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Cell Line:HAEC cells
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Concentration:0.05, 0.12, 0.25, 1 μg/mL
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Incubation Time:1 hour
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Result:Induced production of VEGF which stimulated proliferation of endothelial cells.
In Vivo
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague-Dawley rats (10 to 15-week-age; 270-330 g)[2].
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Dosage:60 μg/kg
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Administration:Intravenous injection; once.
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Result:Increased contraction force, ventricular compliance, and improved heart function.
Reduced the size of no-reflow and infarct.
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Animal Model:Sprague-Dawley rats (350-400 g; crush injury model)[3]
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Dosage:50 µg/per (50 µg/mL, 1 mL for each)
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Administration:Irrigate 1 mL within the vessel lumen (before placement of the last suture); once.
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Result:Showed anticoagulant effect with patency rates of 59%.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 150915-40-5
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Appearance Solid
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Molecular Weight 495.07
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Formel C22H39ClN2O6S
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Color White to off-white
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SMILES
O=S(N[C@H](C(O)=O)CC1=CC=C(OCCCCC2CCNCC2)C=C1)(CCCC)=O.[H]Cl.[H]O[H]
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Synonyms
L700462 hydrochloride monohydrate; MK383 hydrochloride monohydrate
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (6)
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Journal Impact Factor
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Most Recent
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Microsyst Nanoeng
2026 Jan 1;12(1):7. PMID: 41476049
Tirofiban hydrochloride monohydrate purchased from MedChemExpress. Usage Cited in: Microsyst Nanoeng. 2026 Jan 1;12(1):7. [Abstract]
Anti-aggregation efficiency of single-drug combinations for platelets in the combinatorial screening tests for Volunteer 1. For Aspirin (Asp), the concentrations were 2 μM, 4 μM (2 μM + 2 μM), 20 μM, 22 μM (2 μM + 20 μM), and 40 μM (20 μM + 20 μM). For Tirofiban (Tif), the concentrations were 0.2 μM, 0.4 μM (0.2 μM + 0.2 μM), 2 μM, 2.2 μM (0.2 μM + 2 μM), and 4 μM (2 μM + 2 μM). For Ticagrelor, the concentrations were 1 μM, 2 μM (1 μM + 1 μM), 10 μM, 11 μM (10 μM + 1 μM), and 20 μM (10 μM + 10 μM). The results showed that 4 μM Tif (Tirofiban) exhibited the strongest platelet aggregation inhibition.
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Am J Respir Cell Mol Biol
GP IIb/IIIa-ICAM-1 Mediated Platelet-Endothelial Adhesion Exacerbates Pulmonary Hypertension. [Abstract]2025 Feb 28. PMID: 40019848
Tirofiban hydrochloride monohydrate purchased from MedChemExpress. Usage Cited in: Am J Respir Cell Mol Biol. 2025 Feb 28. [Abstract]
CCK8 analysis indicated that the proliferation effect of PH-PLT-EC CM on PASMCs was diminished by Tirofiban (30 μg/mL) or eptifibatide (10 μg/mL). MFI = mean fluorescence intensity.
Tirofiban hydrochloride monohydrate purchased from MedChemExpress. Usage Cited in: Am J Respir Cell Mol Biol. 2025 Feb 28. [Abstract]
Treatment with GPIIb/IIIa antagonists Tirofiban (30 or 300 μg/mL; 45 min) or eptifibatide (1; 10 μg/mL) decreased platelet–EC adhesion. Platelet adhesion was measured by quantifying the remaining fluorescence intensity after the unattached platelets were removed.
Tirofiban hydrochloride monohydrate purchased from MedChemExpress. Usage Cited in: Am J Respir Cell Mol Biol. 2025 Feb 28. [Abstract]
The conditioned medium from EC–platelet cocultures treated with Tirofiban (30 μg/mL), eptifibatide (10 μg/mL), or A-205804 (250 μmol/L) showed reduced PDGF-BB levels.
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Front Pharmacol
Berberine and Its Main Metabolite Berberrubine Inhibit Platelet Activation Through Suppressing the Class I PI3Kβ/Rasa3/Rap1 Pathway. [Abstract]2021 Oct 8:12:734603. PMID: 34690771 -
Mol Divers
Repurposed drugs as PCSK9-LDLR disruptors for lipid lowering and cardiovascular disease therapeutics. [Abstract]2024 Dec 8. PMID: 39645639 -
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Tirofiban hydrochloride monohydrate purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 February 01.
RGD-integrin selectivity of lassotides 36-38 and conjugates 47-49 (shaded), as measured by competitive inhibition vs LAP in ELISA assays against integrins αvβ3, αvβ6 and αvβ8 (as described above) and αvβ1, αvβ5, αIIbβ3, α5β1, and α8β1. *MK-042948 was used as a positive control for all integrin assays except αIIbβ3, where Tirofiban49 was employed.
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 100 mg/mL (201.99 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (5.05 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.05 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protokoll
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Cell migration
Cell migration is a method that plays an important role in wound healing, cell differentiation, embryonic development, etc.
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Reinheit & Dokumentation
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Data Sheet (277 KB)
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SDS (393 KB)
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- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
Verweise
[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. [Content Brief]
[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. [Content Brief]
[3]. Yates YJ, et al. The effect of tirofiban on microvascular thrombosis: crush model. Plast Reconstr Surg. 2005 Jul;116(1):205-8 [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.0199 mL | 10.0996 mL | 20.1992 mL | 50.4979 mL |
| 5 mM | 0.4040 mL | 2.0199 mL | 4.0398 mL | 10.0996 mL | |
| 10 mM | 0.2020 mL | 1.0100 mL | 2.0199 mL | 5.0498 mL | |
| 15 mM | 0.1347 mL | 0.6733 mL | 1.3466 mL | 3.3665 mL | |
| 20 mM | 0.1010 mL | 0.5050 mL | 1.0100 mL | 2.5249 mL | |
| 25 mM | 0.0808 mL | 0.4040 mL | 0.8080 mL | 2.0199 mL | |
| 30 mM | 0.0673 mL | 0.3367 mL | 0.6733 mL | 1.6833 mL | |
| 40 mM | 0.0505 mL | 0.2525 mL | 0.5050 mL | 1.2624 mL | |
| 50 mM | 0.0404 mL | 0.2020 mL | 0.4040 mL | 1.0100 mL | |
| 60 mM | 0.0337 mL | 0.1683 mL | 0.3367 mL | 0.8416 mL | |
| 80 mM | 0.0252 mL | 0.1262 mL | 0.2525 mL | 0.6312 mL | |
| 100 mM | 0.0202 mL | 0.1010 mL | 0.2020 mL | 0.5050 mL |
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