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Entecavir

Catalog No. T0085L CAS 142217-69-4

Synonyms: BMS200475, SQ34676

Entecavir (SQ34676) is a guanosine nucleoside analogue used in the treatment of chronic hepatitis B virus (HBV) infection. Entecavir therapy can be associated with flares of the underlying hepatitis B during or after therapy, but has not been linked to cases of clinically apparent liver injury.

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Entecavir, CAS 142217-69-4

Pack Size	Availability	Price/USD
5 mg	In stock	$ 43.00
10 mg	In stock	$ 79.00
25 mg	In stock	$ 118.00
50 mg	In stock	$ 169.00
100 mg	In stock	$ 297.00
200 mg	In stock	$ 455.00
500 mg	In stock	$ 733.00
1 mL * 10 mM (in DMSO)	In stock	$ 46.00

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Purity: 100%

Purity: 99.72%

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Chemical Properties

Storage & Solubility Information

Description	Entecavir (SQ34676) is a guanosine nucleoside analogue used in the treatment of chronic hepatitis B virus (HBV) infection. Entecavir therapy can be associated with flares of the underlying hepatitis B during or after therapy, but has not been linked to cases of clinically apparent liver injury.
Targets&IC50	HBV (HepG2 cells):3.75 nM(ec50)
In vitro	BMS-200475 demonstrates potent antiviral activity with an EC50 of 3.75 nM against HBV by integrating into the protein primer of HBV, thereby inhibiting the priming step of the virus's reverse transcriptase. Its efficacy is notably reduced against other RNA and DNA viruses[1]. Entecavir, compared to other deoxyguanosine analogs (penciclovir, ganciclovir, lobucavir, and aciclovir) or lamivudine, undergoes more efficient phosphorylation to its active metabolites. Additionally, entecavir has an intracellular half-life of 15 hours[2].
In vivo	Administering BMS-200475 orally on a daily basis in doses between 0.02 and 0.5 mg/kg of body weight for a duration of one to three months significantly decreases the viremia level of woodchuck hepatitis virus (WHV) in chronically infected woodchucks[3].
Cell Research	BMS 200475 is prepared in phosphate-buffered saline (PBS) and diluted with appropriate medium containing 2% fetal bovine serum. HepG2 2.2.15 cells are plated at a density of 5×105 cells per well on 12-well Biocoat collagen-coated plates and are maintained in a confluent state for 2 to 3 days before being overlaid with 1 mL of medium spiked with BMS 200475. Quantification of HBV was performed on day 10[1].

Synonyms	BMS200475, SQ34676
Molecular Weight	277.28
Formula	C12H15N5O3
CAS No.	142217-69-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 55 mg/mL (198.36 mM)

References and Literature

1. Sham, H., Kempf, D., Molla, A., Marsh, K., Kumar, G., & Chen, C. et al. (1998). ABT-378, a Highly Potent Inhibitor of the Human Immunodeficiency Virus Protease. Antimicrobial Agents And Chemotherapy, 42(12), 3218-3224. doi: 10.1128/aac.42.12.3218 2. Xie B, Sun D, Du Y, et al. A two-step lineage reprogramming strategy to generate functionally competent human hepatocytes from fibroblasts[J]. Cell research. 2019: 1.

Citations

1. Xie B, Sun D, Du Y, et al. A two-step lineage reprogramming strategy to generate functionally competent human hepatocytes from fibroblasts. Cell research. 2019: 1. 2. Yang Y, Yan Y, Yin J, et al. Structure-Based Discovery of N-Sulfonylpiperidine-3-carboxamides as Novel Capsid Assembly Modulators for Potent Inhibition of HBV Replication. Viruses. 2022, 14(2): 348. 3. Yin J, Feng Z, Li Z, et al.Synthesis and evaluation of N-sulfonylpiperidine-3-carboxamide derivatives as capsid assembly modulators inhibiting HBV in vitro and in HBV-transgenic mice.European Journal of Medicinal Chemistry.2023: 115141. 4. 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. 5. Yang L, Gong Y, Liu F, et al.A novel phthalazinone derivative as a capsid assembly modulator inhibits hepatitis B virus expression.Antiviral Research.2023: 105763.

Related compound libraries

This product is contained In the following compound libraries：

EMA Approved Drug Library Anti-Cancer Approved Drug Library Anti-Cancer Drug Library Inhibitor Library Anti-Cancer Clinical Compound Library Drug Repurposing Compound Library Clinical Compound Library FDA-Approved Drug Library Anti-COVID-19 Compound Library Nucleotide Compound Library

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Keywords

Entecavir 142217-69-4 Microbiology/Virology HBV BMS200475 BMS-200475 Hepatitis B virus SQ34676 SQ 34676 SQ-34676 BMS 200475 inhibit Inhibitor inhibitor

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