您好,欢迎来到试剂仪器网! [登录] [免费注册]
试剂仪器网
位置:首页 > 产品库 > Tirofiban hydrochloride hydrate(MK-383)
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
Tirofiban hydrochloride hydrate(MK-383)
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 hydrochloride hydrate(MK-383)图片
CAS NO:150915-40-5
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
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.
理化性质和储存条件
Molecular Weight (MW)495.07
FormulaC22H36N2O5S.ClH.H2O
CAS No. 150915-40-5 (HCl hydrate);
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 95 mg/mL (191.89 mM)
Water: 95 mg/mL (191.89 mM)
Ethanol: 95 mg/mL (191.89 mM)
Solubility (In vivo)O=C(O)[C@H](CC1=CC=C(OCCCCC2CCNCC2)C=C1)NS(=O)(CCCC)=O.[H]Cl.[H]O[H]
SynonymsTirofiban; Tirofiban hydrochloride monohydrate; MK-383 Hydrochloride; Aggrastat; L 700462; L-700,462; MK-383; MK 383; MK383
实验参考方法
In Vitro

In vitro activity: 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. Tirofiban (MK-383, Aggrastat) 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 Hydrochloride (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.
Animal model Adult mongrel dogs
Formulation & Dosage Saline;~500 mg/kg; i.p.
References J Med Chem. 1992 Nov 27;35(24):4640-2; J Med Chem. 1994 Aug 5;37(16):2537-51;J Clin Invest. 1997 Dec 1;100(11 Suppl):S57-60.