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Tirofiban(L700462 MK383)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Tirofiban(L700462 MK383)图片
CAS NO:144494-65-5
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)440.6
FormulaC22H36N2O5S
CAS No.144494-65-5 (free base);
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
SMILESO=C(O)[C@H](CC1=CC=C(OCCCCC2CCNCC2)C=C1)NS(=O)(CCCC)=O
SynonymsMK-383 Hydrochloride; Aggrastat; L-700462; MK-383; L 700462; MK 383; L700462; L-700,462; MK383
实验参考方法
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: Tirofiban hydrochloride monohydrate is a potent non-peptide, glycoprotein IIb/IIIa (integrins alphaIIbbetaIII) antagonist IC50 value: Target: integrin IIb/IIIa Tirofiban hydrochloride monohydrate blocks platelet aggregation and thrombus formation. Tirofiban is an antithrombotic used in the treatment of unstable angina. Tirofiban, in a concentration-dependent manner reduced platelet aggregation evoked by ADP (IC50 approximately 70 ng/ml), collagen (IC50 approximately 200 ng/ml), and thrombin (IC50 approximately 5,000 ng/ml).

In VivoTirofiban (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 modelAdult mongrel dogs
Formulation & DosageDissolved in saline; 500 mg/kg; i.p. injection
ReferencesJ Med Chem. 1992 Nov 27;35(24):4640-2; Clin Pharmacol Ther. 1994 Oct;56(4):377-88.