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| 1g |
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Purity: ≥98%
Emtricitabine (BW1592; FTC; Coviracil; Emtriva; Racivir) is a potent nucleoside reverse transcriptase inhibitor (NRTI) with an EC50 of 0.01 µM and has been used for the treatment of both human immunodeficiency virus (HIV) and hepatitis B virus. Emtricitabine is structurally similar to Lamivudine. It is effective at targeting HIV and HBV viruses since these viruses replicate in a reverse transcriptase manner. Studies indicate that the structure of Emtricitabine, specifically the unnatural β-L structural configuration produce greater antiviral effects in vitro on HIV and HBV than other antiviral agents. nucleoside reverse transcriptase inhibitor
| ln Vitro |
Emtricitabine exhibits in vitro efficacy against clinical isolates of HIV-1 as well as laboratory strains of HIV-1 and HIV-2. EC50, or the 50% effective concentration, varies between 0.002 to 1.5 μmol/L based on the cell line and virus isolate employed. When paired with didanosine or zalcitabine, emtricitabine is active in vitro and synergizes with stavudine and zidovudine in vitro [1].
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| ln Vivo |
Emtricitabine was used in toxicity research related to reproduction and development. The daily area under the curve (AUC0→24) for exposure to pregnant animals at oral dosages up to 1000 mg/kg/day once daily is around 60- to 120-fold (mouse to rabbit), greater than the recommended amount for humans ( 200 mg). Emtricitabine had no effect on sperm count, early embryonic development, or fertility in a mouse fertility research. Studies on the embryofetal toxicity of mice and rabbits did not reveal a higher prevalence of abnormalities. Emtricitabine had no effect on the development or fertility of F1 offspring in prenatal or postnatal trials conducted in mice. According to these findings, emtricitabine has a favorable preclinical safety profile for reproduction [2].
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| References |
[1]. Saag MS, et al. Emtricitabine, a new antiretroviral agent with activity against HIV and hepatitis B virus. Clin Infect Dis.?2006 Jan 1;42(1):126-31.
[2]. 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. [3]. Szczech GM, Wang LH, Walsh JP, Reproductive toxicology profile of emtricitabine in mice and rabbits. Reprod Toxicol. 2003 Jan-Feb;17(1):95-108. [4]. 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] |
| Molecular Formula |
C8H10FN3O3S
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|---|---|
| Molecular Weight |
247.25
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| CAS # |
143491-57-0
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| Related CAS # |
Emtricitabine-13C,15N2;1217820-69-3;Emtricitabine-15N,d2;2714436-53-8
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| SMILES |
C1[C@H](O[C@H](S1)CO)N2C=C(C(=NC2=O)N)F
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| InChi Key |
XQSPYNMVSIKCOC-NTSWFWBYSA-N
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| 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
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| Chemical Name |
4-amino-5-fluoro-1-[(2R,5S)-2-(hydroxymethyl)-1,3-oxathiolan-5-yl]pyrimidin-2-one
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| Synonyms |
BW-1592; BW1592; BW 1592; trade names: Coviracil; Emtriva; Racivir; (-)-FTC; W-201247; W-201248; E1007; 24229-EP2298783A1; 24229-EP2314590A1; AB01275429-01; 3B2-0188
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.0445 mL | 20.2224 mL | 40.4449 mL | |
| 5 mM | 0.8089 mL | 4.0445 mL | 8.0890 mL | |
| 10 mM | 0.4044 mL | 2.0222 mL | 4.0445 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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