Darunavir
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
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.
- 1.Velichkovska M, Surnar B, et al. "Targeted Mitochondrial COQ(10) Delivery Attenuates Antiretroviral-Drug-Induced Senescence of Neural Progenitor Cells." Mol Pharm. 2019 Feb 4;16(2):724-736. PMID:30592424
- 2.Lan, Jie, 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. PMID:25149467
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 |
SDF | Download SDF |
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 | 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。 |
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. |
描述 | Darunavir是HIV蛋白酶的抑制剂。 | |||||
靶点 | HIV Protease | |||||
IC50 |
质量控制和MSDS
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