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Purity: ≥98%
Tirofiban (formerly known as L-700462; MK-383; L700462; MK383; Aggrastat) is a novel non-peptide antagonist of glycoprotein IIb/IIIa (integrins alphaIIbbetaIII) that has been approved for use as an antiplatelet drug. Tirofiban is a small molecule inhibitor of the protein-protein interaction between fibrinogen and the platelet integrin receptor GP IIb/IIIa and is the first drug candidate whose origins can be traced to a pharmacophore-based virtual screening lead. Tirofiban Hydrochloride is the hydrochloride salt form of tirofiban, a selective platelet GPIIb/IIIa antagonist which inhibits platelet aggregation. It is more soluable than Tirofiban. Tirofiban inhibits platelet aggregation of gel-filtered platelets induced by 10 μM ADP with IC50 of 9 nM, but the IC50 for inhibition of human umbilical vein adhesion to vitronectin, which depends on ɑvβ3 vitronectin receptors, is 62 μmol/L.
| ln Vitro |
The proliferation of HAEC cells is increased by tirofiban (0.25, 1, 3 μg/mL; 72 hours) [1]. The HUVEC migration scratch is closed in 18 hours by tirofiban (24 hours) [1]. After 30 minutes, tirofiban (0.25, 1 μg/mL; 1 hour) increases endothelial cell proliferation and causes the generation of VEGF [1].
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| ln Vivo |
By raising HR, LVESP, dp/dtmax, and lowering LVEDP, tirofiban (60 μg/kg; IV; once) exhibits activity in enhancing contractility, ventricular compliance, and cardiac function [2]. Tirofiban (60 μg/kg; intravenous injection; once) diminishes the no-reflow region following reperfusion following Acute Myocardial Infarction and increases eNOS activity [2]. In a squeezing model, tirofiban (50 μg/per; irrigation; single dose) showed anticoagulant effects, with a 59% 24-hour patency rate following microvascular anastomosis [3].
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| Cell Assay |
Cell Proliferation Assay[1]
Cell Types: HAEC cells Tested Concentrations: 0.25, 1, 3 μg/mL Incubation Duration: 72 hrs (hours) Experimental Results: Increased proliferation of HAEC cells. Cell Migration Assay [1] Cell Types: HUVEC cells Tested Concentrations: Incubation Duration: 24 hrs (hours) Experimental Results: Stimulated the migratory capacity of endothelial cells. Western Blot Analysis[1] Cell Types: HAEC cells Tested Concentrations: 0.05, 0.12, 0.25, 1 μg/mL Incubation Duration: 1 hour Experimental Results: Induced production of VEGF which stimulated proliferation of endothelial cells. |
| Animal Protocol |
Animal/Disease Models: Male SD (Sprague-Dawley) rats (10 to 15-week-age; 270-330 g)[2].
Doses: 60 μg/kg Route of Administration: intravenous (iv) injection; once. Experimental Results: Increased contraction force, ventricular compliance, and improved heart function. decreased the size of no-reflow and infarct. Animal/Disease Models: SD (Sprague-Dawley) rats (350-400 g; crush injury model)[3] Doses: 50 µg/per (50 µg/mL, 1 mL for each) Route of Administration: Irrigate 1 mL within the vessel lumen (before placement of the last suture); once. Experimental Results: demonstrated anticoagulant effect with patency rates of 59%. |
| References |
[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.
[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. [3]. Yates YJ, et al. The effect of tirofiban on microvascular thrombosis: crush model. Plast Reconstr Surg. 2005 Jul;116(1):205-8. |
| Molecular Formula |
C22H36N2O5S
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| Molecular Weight |
440.6
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| CAS # |
144494-65-5
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| Related CAS # |
Tirofiban hydrochloride monohydrate;150915-40-5;Tirofiban hydrochloride;142373-60-2;Tirofiban-d9;1332075-40-7
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| SMILES |
O=C(O)[ C@H](CC1=CC=C(OCCCCC2CCNCC2)C=C1)NS(=O)(CCCC)=O
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.2270 mL | 1.1348 mL | 2.2696 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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