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Darunavir
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。
Darunavir图片
CAS NO:206361-99-1
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
50mg电议

产品介绍
Darunavir (TMC114) 是一种口服有效的下一代 HIV 蛋白酶抑制剂,对突变病毒和野生型病毒具有相似的抗病毒活性。
Cas No.206361-99-1
别名达芦那韦; TMC114; UIC-94017
化学名(E)-(3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl hydrogen ((2S,3R)-4-(4-amino-N-isobutylphenylsulfonamido)-3-hydroxy-1-phenylbutan-2-yl)carbonimidate
Canonical SMILESCC(CN(S(C1=CC=C(N)C=C1)(=O)=O)C[C@](O)([H])[C@](/N=C(O[C@@]2([H])CO[C@]3([H])[C@@]2([H])CCO3)\O)([H])CC4=CC=CC=C4)C
分子式C27H37N3O7S
分子量547.66
溶解度≥ 22.65mg/mL in DMSO, ≥ 4.94 mg/mL in EtOH with ultrasonic
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Darunavir is an orally-bioavailable non-peptidic inhibitor of human immunodeficiency virus type 1 (HIV-1) protease that selectively inhibits HIV-1 protease enzyme induced cleavage of gag and gag-pol poly-proteins preventing the maturation of virions and also inhibits the dimerization of HIV-1 protease suppressing proteolytic activity and subsequent replication of HIV-1. Study results have shown that darunavir exhibits potent inhibition against HIV-1 with a value of 50% inhibition concentration IC50of 0.003 μmol/L in HIV-1 infected MT-2 cells. Darunavir binds to HIV-1 protease with considerably high affinity and fits closely with the substrate envelop leading to its potent ability to inhibit multidrug-resistant HIV strains.

Reference

[1].McKeage K, Perry CM, Keam SJ. Darunavir: a review of its use in the management of HIV infection in adults. Drugs. 2009;69(4):477-503. doi: 10.2165/00003495-200969040-00007.