| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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Purity: ≥98%
Tirofiban (also known as L700462 or MK383) is a novel non-peptide antagonist of glycoprotein IIb/IIIa (integrins alphaIIbbetaIII) that is used 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 |
HAEC cell proliferation is increased by tirofiban hydrochloride monohydrate (0.25, 1, 3 μg/mL; 72 hours)[1]. Within 18 hours, the scratch caused by HUVEC migration is closed by tirofiban hydrochloride monohydrate (24 hours)[1]. After 30 minutes, tirofiban hydrochloride monohydrate (0.25, 1 μg/mL; 1 hour) stimulates the production of VEGF, which can promote endothelial cell proliferation[1].
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| ln Vivo |
By raising HR, LVESP, dp/dtmax, and lowering LVEDP, tirofiban hydrochloride monohydrate (60 μg/kg; IV; once) improves heart function and increases contraction force and ventricular compliance[2]. After reperfusion following AMI, tirofiban hydrochloride monohydrate (60 μg/kg; iv; once) decreases and increases iNOS activity as well as the area of no-reflow[2]. The crush model demonstrates an anticoagulant effect with patency rates of 59% 24 hours after microvascular anastomosis when tirofiban hydrochloride monohydrate (50 µg/per; irrigate; once) is administered[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 |
| Additional Infomation |
Tirofiban hydrochloride is a hydrochloride. It contains a tirofiban.
Tirofiban Hydrochloride is the hydrochloride salt form of tirofiban, a non-peptide tyrosine derivative with anticoagulant property. Tirofiban antagonizes fibrinogen binding to the platelet cell surface receptor, glycoprotein (GP) IIb/IIIA complex, one of the two purinergic receptors activated by ADP. The antagonism prevents adenylyl cyclase activation, which mediated via GP IIb/IIIa receptor complex, and results in decreased levels of cAMP and thereby interferes with platelet membrane function and subsequent platelet-platelet interaction, release of platelet granule constituents and prolongation of bleeding time. Tyrosine analog and PLATELET GLYCOPROTEIN GPIIB-IIIA COMPLEX antagonist that inhibits PLATELET AGGREGATION and is used in the treatment of ACUTE CORONARY SYNDROME. See also: Tirofiban (has active moiety). |
| Molecular Formula |
C22H36N2O5S.CLH.H2O
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| Molecular Weight |
495.07
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| Exact Mass |
494.221
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| CAS # |
150915-40-5
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| Related CAS # |
Tirofiban;144494-65-5;Tirofiban hydrochloride;142373-60-2
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| PubChem CID |
60946
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| Appearance |
White to off-white solid powder
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| Boiling Point |
611.7ºC at 760 mmHg
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| Melting Point |
135-137ºC
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| Flash Point |
323.7ºC
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| LogP |
5.488
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
14
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| Heavy Atom Count |
32
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| Complexity |
579
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| Defined Atom Stereocenter Count |
1
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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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| InChi Key |
HWAAPJPFZPHHBC-FGJQBABTSA-N
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| InChi Code |
InChI=1S/C22H36N2O5S.ClH.H2O/c1-2-3-16-30(27,28)24-21(22(25)26)17-19-7-9-20(10-8-19)29-15-5-4-6-18-11-13-23-14-12-18;;/h7-10,18,21,23-24H,2-6,11-17H2,1H3,(H,25,26);1H;1H2/t21-;;/m0../s1
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| Chemical Name |
(2S)-2-(butylsulfonylamino)-3-[4-(4-piperidin-4-ylbutoxy)phenyl]propanoic acid;hydrate;hydrochloride
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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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) |
Solubility in Formulation 1: 2.5 mg/mL (5.05 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.05 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.05 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*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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