Darunavir

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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。

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

化学性质

Physical Appearance	A solid
Storage	Store at -20°C
M.Wt	547.66
Cas No.	206361-99-1
Formula	C₂₇H₃₇N₃O₇S
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
Canonical SMILES	CC(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
运输条件	蓝冰运输或根据您的需求运输。
一般建议	为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。

资料参考

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.

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-1_LAIin 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