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Darunavir

达芦那韦
Catalog No.
A8206
HIV-1蛋白酶抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 1,272.00
现货
5mg
¥ 545.00
现货
50mg
¥ 3,000.00
现货

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A

背景

Darunavir(达芦那韦)是一种可口服的人类免疫缺陷病毒1型(HIV-1)蛋白酶非肽抑制剂,选择性抑制HIV-1蛋白酶诱导的gag和gag-pol聚蛋白的切除,阻止病毒粒子的成熟;也抑制HIV-1蛋白酶的二聚化,从而抑制蛋白水解活性和随后的HIV-1复制。研究结果表明,在HIV-1感染的MT-2细胞中,darunavir有效抑制HIV-1,IC50值为0.003 μmol/L。Darunavir与HIV-1蛋白酶高亲和性地结合,紧密围绕其底物,导致其有效抑制多药耐药性HIV毒株。

参考文献:
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.

文献引用

化学属性

Physical AppearanceA solid
StorageStore at -20°C
M.Wt547.66
Cas No.206361-99-1
FormulaC27H37N3O7S
Solubility≥22.65 mg/mL in DMSO; insoluble in H2O; ≥4.94 mg/mL in EtOH with ultrasonic
Chemical Name(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
SDFDownload SDF
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
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试验操作

Cell experiment:[1]

Cell lines

MT-2 cells and phytohemagglutinin-activated peripheral blood mononuclear cells (PHA-PBMCs)

Reaction Conditions

3 nM darunavir (IC50 in MT-2 cells) for 7 d incubation

Applications

Darunavir was active against HIV-1LAI in MT-2 cells (IC50 = 3 nM) with a 50% cytotoxic concentration (CC50) of 74.4 μM. Darunavir was also active against wild-type and multidrug-resistant clinical isolates of HIV-1 in PHA-PBMCs, with IC50 values being 3 and 3 ~ 29 nM, respectively.

Note

The technical data provided above is for reference only.

References:

1. Koh Y, Nakata H, Maeda K, et al. Novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI) UIC-94017 (TMC114) with potent activity against multi-PI-resistant human immunodeficiency virus in vitro. Antimicrobial Agents and Chemotherapy, 2003, 47(10): 3123-3129.

生物活性

描述 Darunavir是HIV蛋白酶的抑制剂。
靶点 HIV Protease          
IC50            

质量控制

化学结构

Darunavir

相关生物数据

Darunavir
Darunavir had no effect on provirus activation by provirus stimulants, as percentage of Env-positive cells was not altered [1].
1. Lan J, Yang K, Byrd D, et al. Provirus Activation Plus CD59 Blockage Triggers Antibody-Dependent Complement-Mediated Lysis of Latently HIV-1–Infected Cells. The Journal of Immunology, 2014: 1303030.

相关生物数据

Darunavir