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Emtricitabine(BW1592)
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。
Emtricitabine(BW1592)图片
CAS NO:143491-57-0
规格:≥98%
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议
1g电议
10g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)247.25
FormulaC8H10FN3O3S
CAS No.143491-57-0
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 49 mg/mL (198.2 mM)
Water: 49 mg/mL (198.2 mM)
Ethanol: 9 mg/mL (36.4 mM)
Other infoChemical Name: 4-amino-5-fluoro-1-[(2R,5S)-2-(hydroxymethyl)-1,3-oxathiolan-5-yl]pyrimidin-2-one
InChi Key: XQSPYNMVSIKCOC-NTSWFWBYSA-N
InChi Code: InChI=1S/C8H10FN3O3S/c9-4-1-12(8(14)11-7(4)10)5-3-16-6(2-13)15-5/h1,5-6,13H,2-3H2,(H2,10,11,14)/t5-,6+/m0/s1
SMILES Code: C1[C@H](O[C@H](S1)CO)N2C=C(C(=NC2=O)N)F
SynonymsBW-1592; BW1592; BW 1592; trade names: Coviracil; Emtriva; Racivir; (-)-FTC; W-201247; W-201248; E1007; 24229-EP2298783A1; 24229-EP2314590A1; AB01275429-01; 3B2-0188
实验参考方法
In Vitro

In vitro activity: Emtricitabine moderately reduces hepatocyte proliferation independent of effects on mtDNA in HepG2 human hepatoma cells. Emtricitabine plus tenofovir slightly reduced cell proliferation without affecting mitochondrial parameters. Emtricitabine efficiently converts to their active metabolites in PBMCs and CEM cells. Emtricitabine combined with Tenofovir displays additive to synergistic activity against HIV replication in PBMCs and results in strongly synergistic anti-HIV activity in MT-2 cells against both wild-type and mutant virus. Emtricitabine demonstrates antiviral activity against laboratory adapted strains of HIV-1 and HIV-2 in various cell system. Emtricitabine also exhibits antiviral activity in cell culture against feline and simian immuno-deficiency viruses (SIVs). Emtricitabine consistently exhibits up to 10-fold greater activity than lamivudine against all viruses tested in all T-cell lines. Emtricitabine generally demonstrates greater potency in vitro in human PBMCs than in MT-4 lines. Emtricitabine also exhibits anti-HBV activity in vitro (EC50, 0.01–0.04 μM) that is comparable to the anti-HBV activity of 3TC. Emtricitabine is approximately fourfold more active than 3TC in assays in the transformed T-cell line MT-4 infected with HIV-(1IIIB), whereas Zidovudine is more active than Emtricitabine. Emtricitabine, Lamivudine and Zidovudine are equally active against a panel of eight primary HIV-1 isolates from antiretroviral-naive subjects in PBMCs.


Cell Assay: Emtricitabine, an antiretroviral agent is used to evaluate degradation pathways under different stress conditions in order to identify degradation products as prescribed by ICH guidelines. Emtricitabine degrades over 51%, 13% and 53% during acid, base and oxidative degradation respectively followed by formation of three major degradation products (Degradant-I to Degradant-III).

In VivoReproductive and developmental toxicology studies are conducted with emtricitabine. Oral doses up to 1000 mg/kg/day provided daily area under the curve (AUC0→24) exposure to pregnant animals approximately 60- (mice) to 120-fold (rabbits) higher than that in humans at the recommended dose of 200 mg given once per day. In a mouse fertility study, emtricitabine had no effect on fertility, sperm count, or early embryonic development. There is no increased incidence of malformations in mouse and rabbit embryofetal toxicology studies. The development and fertility of F1 progeny are unaffected by emtricitabine in a mouse pre- and post-natal study. These data demonstrate a favorable pre-clinical reproductive safety profile for emtricitabine
Animal modelMouse
Formulation & DosageOral
ReferencesAntivir Ther. 2007;12(7):1075-85; Antivir Ther. 2006;11(3):377-84.