那罗帕西 T68002

Product Introduction
Bioactivity


英文名: Naroparcil

描述: Naroparcil 是一种可口服的硫代苷类化合物，是一种 4-甲基伞形 β-D-木糖苷类似物，在静脉血栓形成（颈静脉）的Wessler淤滞模型中显示出抗血栓形成作用。Naroparcil 增强了凝血酶/肝素辅因子II复合物的形成，诱导了处理兔血浆中硫酸皮肤素样物质的出现，但减少了与（125I）-人α-凝血酶孵育的血浆中的凝血酶/抗凝血酶III复合物的形成。

体内活性: Naroparcil attenuated thrombus development in a Wessler stasis model of venous thrombosis (jugular vein) employing bovine factor Xa as a thrombogenic stimulus giving ED50 values of 21.9 mg/kg and 36.0 mg/kg after respectively i.v. and p.o.. Venous antithrombotic activity was maximal 2-3 h after i.v. administration and 4-8 h after oral administration. Four hours after the oral administration of maximal antithrombotic (Wessler model, factor Xa) doses (100 and 400 mg/kg), naroparcil had no significant effect on bleeding time. In platelet-poor plasma obtained from animals treated 4 h previously with various doses (25 to 400 mg/kg) of naroparcil, there was no detectable anti-factor Xa nor antithrombin activity. Similarly, naroparcil had no effect on APTT nor on thrombin time. A sensitized thrombin time (to about 35 s) was modestly but significantly increased following oral administration of the compound at 400 mg/kg. However, thrombin generation by the intrinsic pathway was reduced in a dose-related manner, with maximal reduction being 65% at 400 mg/kg. The same dose of naroparcil enhanced the formation of thrombin/heparin cofactor II complexes at the expense of thrombin/antithrombin III complexes in plasma incubated with (125I)-human alpha-thrombin and induced the appearance of dermatan sulfate-like material in the plasma of treated rabbits, as measured by a heparin cofactor II-mediated thrombin inhibition assay.[1]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 50 mg/mL (129.04 mM)


相关产品: Pirodomast | Bivalirudin | Thrombin receptor peptide ligand | Proflavine Hemisulfate | Dabigatran Etexilate Mesylate | Ozagrel | Flovagatran | Efegatran sulfate | Z-Gly-Pro-Arg-4MβNA | Protamine sulfate

相关库: Bioactive Compounds Library Max | Bioactive Compound Library

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