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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
规格:≥98%
包装与价格:
包装价格(元)
1mg电议
2mg电议
5mg电议
10mg电议
50mg电议
250mg电议
500mg电议
1g电议
2g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)547.66
FormulaC27H37N3O7S
CAS No.206361-99-1 (free); 635728-49-3 (Ethanolate); 2281870-65-1 (dihydrate);
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 10 mM
Water: <1 mg/mL
Ethanol: <1 mg/mL
SMILES CodeO=C(O[C@@H]1[C@@]2([H])[C@@](OCC2)([H])OC1)N[C@@H](CC3=CC=CC=C3)[C@H](O)CN(S(=O)(C4=CC=C(N)C=C4)=O)CC(C)C
SynonymsDarunavir; TMC-114; TMC114; TMC 114; UIC-94017; UIC 94017; UIC94017; Trade name: Prezista.
实验参考方法
In Vitro

In vitro activity: Darunavir displays potent activity against HIV strains resistant to other available protease inhibitor. Darunavir inhibits P-glycoprotein-mediated efflux of calcein-acetoxymethyl ester in L-MDR1 cells with the inhibitory potency of 121 mM. Darunavir is a protein inhibits that mimics the phenylalanine sequences at positions 167 and 168 of the gag-pol polypeptide and binds to the active sites of the HIV protease, thereby inhibiting its activity. Darunavir blocks the infectivity and replication of each of the HIV-1 variants at concentrations up to 5 μM. Darunavir shows strong ARV activity against a selected panel of 19 recombinant clinical isolates carrying multiple protease mutations conferring resistance to an average of five other protien inhibitors. Darunavir inhibits 75% of 1501 PI-resistant viruses tested with a half maximal effective concentration (EC50) of < 10 nM.


Kinase Assay: Darunavir has a Ki of 1 nM for wild type HIV-1 protease.


Cell Assay: In an in vitro study in MT-2 cells, the potency of darunavir is greater than that of saquinavir, amprenavir, nelfinavir, indinavir, lopinavir and ritonavir. Darunavir is primarily metabolized by the hepatic cytochrome P450 (CYP) enzymes, primarily CYP3A. The ‘boosting’ dose of ritonavir acts an an inhibitor of CYP3A, thereby increasing darunavir bioavailability

In VivoDarunavir is effective against wild-type and PI-resistant HIV, and has an oral bioavailability of 37%. It is often used in combination with ritonavir, which increases the bioavailability to 82%
Animal model N/A
Formulation & Dosage N/A
ReferencesBiol Pharm Bull. 2009 Sep;32(9):1588-93; Expert Opin Pharmacother. 2007 Aug;8(12):1951-64.
生物活性
Biological activity-darunavir