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| 25mg |
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| 50mg |
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| 100mg |
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Purity: ≥98%
Tirofibanhydrochloride (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 |
Tirofiban hydrochloride (0.25, 1, 3 μg/mL; 72 hours) promotes proliferation of HAEC cells[1]. Tirofiban hydrochloride (24 hours) closes the scratch of HUVECs migrating within 18 hours[1]. Tirofiban hydrochloride (0.25, 1 μg /mL; 1 hour) stimulates production of VEGF after 30 minutes which can boost proliferation of endothelial cells[1].
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|---|---|
| ln Vivo |
By raising HR, LVESP, dp/dtmax, and lowering LVEDP, tirofiban hydrochloride (60 μg/kg; IV; once) improves heart function and increases contraction force and ventricular compliance[2]. After reperfusion following AMI, tirofiban hydrochloride (60 μg/kg; iv; once) lowers and increases iNOS activity as well as the area of no-reflow[2]. In the crush model, tirofiban hydrochloride (50 µg/per; irrigation; once) exhibits an anticoagulant action with 59% patency rates 24 hours 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 |
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| 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 |
C22H37CLN2O5S
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|---|---|
| Molecular Weight |
477.0576
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| Exact Mass |
494.221
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| CAS # |
142373-60-2
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| Related CAS # |
Tirofiban hydrochloride monohydrate;150915-40-5;Tirofiban;144494-65-5
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| PubChem CID |
60946
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| Appearance |
Typically exists as solid at room temperature
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| Boiling Point |
611.7ºC at 760mmHg
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| Melting Point |
223-225ºC
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| Flash Point |
323.7ºC
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| Vapour Pressure |
8.09E-16mmHg at 25°C
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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 |
Cl[H].S(C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H])(N([H])[C@]([H])(C(=O)O[H])C([H])([H])C1C([H])=C([H])C(=C([H])C=1[H])OC([H])([H])C([H])([H])C([H])([H])C([H])([H])C1([H])C([H])([H])C([H])([H])N([H])C([H])([H])C1([H])[H])(=O)=O
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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 |
Tirofiban; Tirofiban hydrochloride; MK-383 Hydrochloride;Aggrastat; L 700462; L-700,462; MK-383; MK 383; MK383
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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 |
| 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) |
DMSO:95 mg/mL (191.89 mM)
Water:95 mg/mL (191.89 mM)
Ethanol:95 mg/mL (191.89 mM)
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|---|---|
| Solubility (In Vivo) |
O=C(O)[C@H](CC1=CC=C(OCCCCC2CCNCC2)C=C1)NS(=O)(CCCC)=O.[H]Cl (Please use freshly prepared in vivo formulations for optimal results.)
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0962 mL | 10.4809 mL | 20.9617 mL | |
| 5 mM | 0.4192 mL | 2.0962 mL | 4.1923 mL | |
| 10 mM | 0.2096 mL | 1.0481 mL | 2.0962 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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