
Amount : | 10 mg |
Purification : | ≥98% |
Content : | Grazoprevir is supplied as a crystalline solid. |
Storage condition : | Store at -20°C. |
Alternative Name : | MK-5172 |
Molecular Formula:C38H50N6O9S
Molecular Weight:766.9
Grazoprevir is a pan-genotypic protease inhibitor that binds to hepatitis C virus (HCV) non-structural protein 3/4A (NS3/4A), a serine protease essential for viral replication.Grazoprevir has potent in vitro activity against major HCV genotypes (Kis = 0.1, 0.1, 0.08, 0.15, and 0.9 nM for genotypes 1a, 1b, 2a, 2b, and 3a, respectively) and common resistance genotypes (Kis = 0.07, 0.14, and 0.30 nM for genotypes 1b R155K, D165V, and D168Y, respectively). Grazoprevir inhibits the NS3/4A protease in an in vitro replicon system with EC50 values of 2 and 8 nM for genotypes 1a and 2a, respectively. Formulations containing grazoprevir are used in combination therapies to treat HCV.
For Research Use Only. Not for use in diagnostic/therapeutics procedures.
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《血管紧张素转换酶抑制剂在心血管病中应用的中国专家共识》.PDF(242.69k)
1.对于抑制剂筛选工作(求ic50)是不是体系内酶与底物的量(底物应该是过量的)对实验结果影响不大。
2.如果要求算Km值,是不是需要知道反应产物的绝对量。反应时间文献上都是5分钟,反应速度就用反应产物量除以反应时间即可。
3.酶是进口分装的,规格5U,一次用不完,用PBS稀释后如何保存
谢谢
2、可逆抑制剂:包括
a、竞争性抑制剂,抑制剂与底物竞争性结合酶反应中心,使Km增大,而Vmax不变 b、非竞争性抑制剂,酶与抑制剂结合后还能与底物结合,但活性降低,使Vmax减小,而Km不变
c、反竞争性抑制剂,酶只能与底物结合后才能与抑制剂结合,Vmax与Km都减小
可逆抑制剂可用透析等方法除去,使酶恢复作用
1、测定酶比活力:底物需要过量么?测定时间多长?是否可以加入过量的底物,然后测定3min吸光度的增加值,从吸光度的变化值计算比活力。
2、在酶抑制剂筛选的过程中,是否需要保证底物过量?还是要水浴一定时间让反应完全?我看到文献说用终浓度为0.1μmol/mL的底物,终浓度为45U/ml的酶,我想问,假设总体积为1ml,那么终浓度为45U/ml的酶岂不是每分钟能转化4.8μmol的底物?那么0.1μmol/mL的底物不就几秒钟就反应完了?那么怎么测定初速度?

