Amount : | 10 mg |
Purification : | ≥98% |
Content : | Paritaprevir is supplied as a solid. |
Storage condition : | Store at -20°C, product is stable for at least two years. |
Alternative Name : | ABT-450 |
Molecular Formula:C40H43N7O7S
Molecular Weight:765.9
Paritaprevir is an orally bioavailable, direct-acting inhibitor of the hepatitis C virus (HCV) non-structural 3/4A (NS3/4A) serine protease.It inhibits HCV replication in stable Huh7-derived replicon cell lines infected with subgenomic genotypes 1a, 1b, 2a, 3a, 4a, and 6a (EC50s = 1, 0.21, 5.3, 19, 0.09, and 0.69 nM, respectively). It also inhibits replicons from clinical isolates of genotypes 1a (EC50s = 0.43-1.87 nM) and 1b (EC50s = 0.033-0.087 nM). Formulations containing paritaprevir in combination with ombitasvir, ritonavir, and dasabuvir with and without ribavirin have been used in the treatment of chronic HCV genotype 1 infection.
For Research Use Only. Not for use in diagnostic/therapeutics procedures.
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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.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
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?
《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)
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