产品说明书

Emtricitabine

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Chemical Structure| 143491-57-0 同义名 : BW1592;BW 524W91;Emtriva.;DRG-0208;dOTFC;Coviracil;524W91;2-FTC;FTC
CAS号 : 143491-57-0
货号 : A188531
分子式 : C8H10FN3O3S
纯度 : 98%
分子量 : 247.247
MDL号 : MFCD00870151
存储条件：

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(424.68 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 25 mg/mL(101.11 mM)
动物实验配方：
生物活性
描述 Emtricitabine is a nucleoside reverse transcriptase inhibitor (NRTI) with an EC50 of 0.01 µM in PBMC cell. It is an antiviral drug for the treatment of HIV infection. Emtricitabine has in vitro activity against both laboratory strains of HIV-1 and HIV-2 and clinical isolates of HIV-1. The 50% effective concentration (EC50) ranges from 0.002 to 1.5 µ mol/L, depending on the viral isolate and cell line used. Emtricitabine demonstrates in vitro synergy with zidovudine and stavudine and additive in vitro activity when combines with zalcitabine or didanosine[3]. 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[4].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
HeLa P4/R5 cells Function assay Antiviral activity against HIV1 infected in human HeLa P4/R5 cells assessed as inhibition of viral replication, IC50=0.17 μM 19596885
HepAD38 cell Function assay Inhibition of hepatitis B virus replication in the HepAD38 cell line, ED50=0.03 μM 11128652
HepG2 cells Cytotoxicity assay 9 days Cytotoxicity against human HepG2 cells after 9 days by MTT assay, IC50=27.7 μM 17888662
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.04mL

0.81mL

0.40mL

20.22mL

4.04mL

2.02mL

40.45mL

8.09mL

4.04mL
参考文献

[1]Venhoff N, Setzer B, et al. Mitochondrial toxicity of tenofovir, emtricitabine and abacavir alone and in combination with additional nucleoside reverse transcriptase inhibitors. Antivir Ther. 2007;12(7):1075-85.

[2]Borroto-Esoda K, Vela JE, et al. In vitro evaluation of the anti-HIV activity and metabolic interactions of tenofovir and emtricitabine. Antivir Ther. 2006;11(3):377-84.

[3]Saag MS. Emtricitabine, a new antiretroviral agent with activity against HIV and hepatitis B virus. Clin Infect Dis. 2006;42(1):126-131.

[4]Xu P, Wang Y, Qin Z, et al. Combined Medication of Antiretroviral Drugs Tenofovir Disoproxil Fumarate, Emtricitabine, and Raltegravir Reduces Neural Progenitor Cell Proliferation In Vivo and In Vitro. J Neuroimmune Pharmacol. 2017;12(4):682-692.