Entecavir

製品コードS5246 バッチS524601

化学情報

	Synonyms	BMS200475,SQ34676	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₁₂H₁₅N₅O₃
	分子量	277.28	CAS No.	142217-69-4
Solubility (25°C)*	体外	DMSO	55 mg/mL (198.35 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Entecavir(BMS200475,SQ34676), a new deoxyguanine nucleoside analogue, is a selective inhibitor of the replication of the hepatitis B virus (HBV).
in vitro	For treatment of hepatitis B virus, combinations of ETV with each of the other HBV NRTI antivirals, adefovir, tenofovir, and lamivudine at 10 times their respective C^max levels fails to result in cellular or mitochondrial toxicity, and displays no DNA polymerase gamma inhibition.^[1]
in vivo	Treatment with Entecavir in combination with AIC649, Induces tightly regulated Immunological and virological responses during active and maintenance ereatment in the woodchuck model of chronic hepatitis B.

プロトコル(参考用のみ)

細胞アッセイ	細胞株	HepG2 cells
	濃度	0.034 - 3.4 μM
	反応時間	15 days
	実験の流れ	HepG2 cells (2.7 × 10₆) are seeded onto collagen I-coated T75 flasks. Cultures are exposed to compounds for a total of 15 days, reseeding every 5 days to the original cell density. In addition, media and compounds are also replaced 3 days after seeding. This schedule results in replacement of media containing fresh compound on days 1, 3, 5, 8, 10, and 13. Cells and culture supernatants are harvested and assayed on days 5, 10, and 15.
動物実験	動物モデル	Woodchucks inoculated with strain 7 of WHV
	投薬量	0.2 mg/kg
	投与方法	p.o.

参考

[1] Mazzucco CE, et al. Antimicrob Agents Chemother. 2008 Feb;52(2):598-605.

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

A therapeutic hepatitis B mRNA vaccine with strong immunogenicity and persistent virological suppression [ NPJ Vaccines, 2024, 9(1):22]	PubMed: 38310094
Preclinical Antiviral and Safety Profiling of the HBV RNA Destabilizer AB-161 [ Viruses, 2024, 16(3)323]	PubMed: 38543689
Reverse Transcriptase Inhibition Disrupts Repeat Element Life Cycle in Colorectal Cancer [ Cancer Discov, 2022, candisc.1117.2021]	PubMed: 35320348
In vitro investigation of HBV clinical isolates from Chinese patients reveals that genotype C isolates possess higher infectivity than genotype B isolates [ Virol Sin, 2022, S1995-820X(22)00062-1]	PubMed: 35314401
Rapamycin inhibits hepatitis B virus covalently closed circular DNA transcription by enhancing the ubiquitination of HBx [ Front Microbiol, 2022, 13:850087]	PubMed: 36033851
Genotoxicity assessment of potentially mutagenic nucleoside analogues using ToxTracker® [ Toxicol Lett, 2022, 362:50-58]	PubMed: 35569722
Preclinical characterization of AB-506, an inhibitor of HBV replication targeting the viral core protein [ Antiviral Res, 2021, 197:105211]	PubMed: 34826506
A cell-based assay to discover inhibitors of SARS-CoV-2 RNA dependent RNA polymerase [ Antiviral Res, 2021, S0166-3542(21)00068-1]	PubMed: 33894278
Treatment with the Immunomodulator AIC649 in Combination with Entecavir Produces Antiviral Efficacy in the Woodchuck Model of Chronic Hepatitis B [ Viruses, 2021, 13(4)648]	PubMed: 33918831
Anti-HBV therapeutic potential of small molecule 3,5,6,7,3',4'-Hexamethoxyflavone in vitro and in vivo [ Virology, 2021, 560:66-75]	PubMed: 34051476

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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