Tirofiban hydrochloride monohydrate

Research use only, not for human use.

A potent, selective inhibitor of the platelet fibrinogen receptor GPIIb/IIIa with IC50 of 9 nM.

A potent, selective inhibitor of the platelet fibrinogen receptor GPIIb/IIIa with IC50 of 9 nM, inhibition of platelet aggregation; displays > 24,000-fold over human umbilical vein endothelial cell fibrinogen receptors; inhibits ex vivo platelet aggregation induced by ADP in anesthetized dogs.Thrombosis Approved(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.(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.

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. 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.

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. 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%.

L-700462 | MK-383 | MK-0383

Cell Cycle/DNA Damage

Integrin

GPIIb/IIIa

Cardiovascular Disease

Thrombosis

150915-40-5

495.0728

C22H39ClN2O6S

>98% (HPLC)

DMSO: 12 mg/mL

CCCCS(=O)(=O)N[C@@H](CC1=CC=C(C=C1)OCCCCC2CCNCC2)C(=O)O.O.Cl

L-Tyrosine, N-(butylsulfonyl)-O-[4-(4-piperidinyl)butyl]-, hydrochloride, hydrate (1:1:1)

(-20℃)

With Ice Pack

≥ 2 years