product name Tirofiban
Description: Tirofiban (also known as MK-383) is a potent and selective palate GPIIb/IIIa antagonist which inhibits platelet aggregation with IC50 of 9 NM. Tirofiban is an antiplatelet drug that belongs to a class of glycoprotein IIb/IIIa inhibitors. Tirofiban is indicated to reduce the rate of thrombotic cardiovascular events (combined endpoint of death, myocardial infarction, or refractory ischemia/repeat cardiac procedure) in patients with non-ST elevation acute coronary syndrome (NSTE-ACS).
References: J Med Chem. 1992 Nov 27;35(24):4640-2; Clin Pharmacol Ther. 1994 Oct;56(4):377-88.
440.6
Formula
C22H36N2O5S
CAS No.
144494-65-5
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: <1 mg/mL
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
MK-383
other peoduct :
| In Vitro |
In vitro activity: Tirofiban (MK-383, Aggrastat) is a nonpeptide derivative of tyrosine that selectively inhibits the GP-IIb/IIIa receptor, with minimal effects on the ɑvβ3 vitronectin receptor. It 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. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | Tirofiban (10 to 500 mg/kg or 360-min continuous i.v. infusions of 1 to 10 micrograms/kg/min) inhibits platelet aggregation responses to ADP and collagen in canine models. When administered to humans at 0.15μg/kg/min for 4 h, Tirofiban produced a 2.5-fold increase in bleeding time and 97% inhibition of ADP-induced platelet aggregation. |
| Animal model | Adult mongrel dogs |
| Formulation & Dosage | Dissolved in saline; 500 mg/kg; i.p. injection |
| References | J Med Chem. 1992 Nov 27;35(24):4640-2; Clin Pharmacol Ther. 1994 Oct;56(4):377-88. |
