| Description | Emtricitabine (FTC) (FTC), a nucleoside reverse transcriptase inhibitor, exhibits inhibition activity against human immunodeficiency virus (HIV) and hepatitis B virus. |
| In vivo | Reproductive and developmental toxicology studies are performed with emtricitabine. Oral doses up to 1000 mg/kg/day provided a 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 shows a favorable pre-clinical reproductive safety profile for emtricitabine[6]. |
| Cell experiments | EA.hy926 cells were plated in a 12-, 24- or 96-well plates and grown in DMEM media supplemented with 3% FCS. Endothelial cells from PARP+/+and PARP-/- mice were isolated and cultured. Cell viability was determined by the reduction of yellow MTT into a purple formazan product by mitochondrial dehydrogenases of metabolically active cells. Following the treatment period, the experimental medium was removed and 100 μL MTT (1 mg/mL) added. After 1 h incubation, the MTT solution was carefully removed and the purple crystals were solubilized in 100 μL of DMSO. The DMSO was transferred to an ELISA plate and absorbance measured at 550 nm with a 620 nm[3]. |
| Target activity | NRTI:0.01 µM(EC50) |
| Synonyms | 恩曲他滨, FTC, Emtriva, BW1592 |
| molecular weight | 247.25 |
| Molecular formula | C8H10FN3O3S |
| CAS | 143491-57-0 |
| Storage | store at low temperature,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 50 mg/mL (202.22 mM) |
| References | 1. Venhoff N, et al. Antivir Ther, 2007, 12(7), 1075-1085. 2. Borroto-Esoda K, et al. Antivir Ther, 2006, 11(3), 377-384. 3. Richman DD, et al. Antivir Ther, 2001, 6(2), 83-88. 4. Saag MS, et al. Clin Infect Dis, 2006, 42(1), 126-131. 5. Hazen R, et al. J Acquir Immune Defic Syndr, 2003, 32(3), 255-258. 6. Xu P, 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 Dec;12(4):682-692. 7. Faltz M, et al. Effect of the Anti-retroviral Drugs Efavirenz, Tenofovir and Emtricitabine on Endothelial Cell Function: Role of PARP. Cardiovasc Toxicol. 2017 Jan 3. [Epub ahead of print] |
| Citations | 1. Bao H, Yan J, Huang J, et al.Activation of endogenous retrovirus triggers microglial immuno-inflammation and contributes to negative emotional behaviors in mice with chronic stress.Journal of Neuroinflammation.2023, 20(1): 1-16. |