Emtricitabine

SKU: orb1300973

Description

Emtricitabine is a potent nucleoside reverse transcriptase inhibitor (NRTI) effective against HIV and HBV, demonstrating an EC50 of 0.01 µM in PBMC assays. It is widely used in both in vitro virology studies and in vivo models to investigate antiviral mechanisms and therapeutic strategies for retroviral infections.

Research Area

Infectious Disease & Virology, Metabolism Research, Pharmacology & Drug Discovery, Protein Biochemistry

Key Properties

• CAS Number: 143491-57-0
• MW: 247.25
• Purity: 99.15% (May vary between batches)
• Formula: C₈H₁₀FN₃O₃S
• SMILES: Nc1nc(=O)n(cc1F)[C@@H]1CS[C@H](CO)O1
• Target: HIV Protease,Endogenous Metabolite,Reverse Transcriptase
• Solubility: DMSO:237 mg/mL (958.54 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (20.22 mM)

Bioactivity

• Target IC50:
  NRTI:0.01 µM(EC50)
• In Vivo:
  Reproductive and developmental toxicology studies conducted on emtricitabine show a favorable pre-clinical safety profile. When administered orally at doses up to 1000 mg/kg/day, pregnant animals experienced emtricitabine exposure levels (AUC0→24) approximately 60-fold (in mice) to 120-fold (in rabbits) higher than the human exposure at the recommended 200 mg daily dosage. Findings from a mouse fertility study indicate that emtricitabine does not impact fertility, sperm count, or early embryonic development. Additionally, there was no observed increase in malformations in mouse and rabbit embryofetal toxicology studies, nor did emtricitabine affect the development and fertility of the F1 progeny in a mouse pre- and post-natal study. These results underscore emtricitabine's lack of adverse effects on reproductive and developmental outcomes.
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• In Vitro:
  METHODS: Vero E6 cells were treated with Emtricitabine (25, 50, 100 μM), and the SARS-CoV-2 titers obtained before and after treatment were measured. The MTT assay was used to evaluate the cytotoxicity of Emtricitabine against Vero E6 cells. RESULTS Emtricitabine showed anti-SARS-CoV-2 activity at 100 μM (59.6%), 50 μM (43.4%), and 25 μM (33.3%).
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• Cell Research:
  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.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

ReverseTranscriptase, Reverse Transcriptase, BW 1592, BW1592, BW-1592, Inhibitor, inhibit, Human immunodeficiency virus, HIVProtease, HIV Protease, HIV, Emtricitabine, Emtriva, FTC

Compound Identifiers

PubChem CID

60877