Telbivudine

製品コードS1651 バッチS165102

印刷

化学情報

Synonyms

NV 02B

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₁₀H₁₄N₂O₅

分子量

242.23

CAS No.

3424-98-4

Solubility (25°C)*

体外

DMSO (warmed with 50ºC water bath)

48 mg/mL (198.15 mM)

Water (warmed with 50ºC water bath)

48 mg/mL (198.15 mM)

Ethanol (warmed with 50ºC water bath)

2 mg/mL (8.25 mM)

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension

CMC-NA

≥5mg/ml

Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

* <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	Telbivudine(NV 02B) is a potent, and selective HBV reverse transcriptase inhibitor, used to treat HBV infection.
in vitro	Telbivudine shows potent, selective, and specific antiviral activity against HBV and other hepadna viruses. This compound is phosphorylated by intracellular thymidine kinases to the active triphosphate form, which has an intracellular half-life of 14 hours. Its 5′-triphosphate inhibits HBV DNA polymerase (reverse transcriptase) by competing with the natural substrate, dTTP. ^[1] This chemical significantly increases the production of tumour necrosis factor-alpha and interleukin-12 in MHV-3-induced macrophages. It significantly elevates serum levels of interferon-gamma. This treatment enhances the ability of T cells to undergo proliferation and secrete cytokines but does not affect cytotoxicity of infected hepatocytes. It suppresses programmed death ligand 1 expression on T cells. ^[2] The compound remains active as shown by respective fold-changes of 0.5 (N236T) and 1.0 (A181V and A194T). It is not active against HBV strains bearing lamivudine mutations L180M/M204V/I but remains active against the M204V single mutant in vitro, potentially explaining the difference in resistance profiles between telbivudine and lamivudine. ^[3]

製品説明

Telbivudine(NV 02B) is a potent, and selective HBV reverse transcriptase inhibitor, used to treat HBV infection.

in vitro

Telbivudine shows potent, selective, and specific antiviral activity against HBV and other hepadna viruses. This compound is phosphorylated by intracellular thymidine kinases to the active triphosphate form, which has an intracellular half-life of 14 hours. Its 5′-triphosphate inhibits HBV DNA polymerase (reverse transcriptase) by competing with the natural substrate, dTTP. ^[1] This chemical significantly increases the production of tumour necrosis factor-alpha and interleukin-12 in MHV-3-induced macrophages. It significantly elevates serum levels of interferon-gamma. This treatment enhances the ability of T cells to undergo proliferation and secrete cytokines but does not affect cytotoxicity of infected hepatocytes. It suppresses programmed death ligand 1 expression on T cells. ^[2] The compound remains active as shown by respective fold-changes of 0.5 (N236T) and 1.0 (A181V and A194T). It is not active against HBV strains bearing lamivudine mutations L180M/M204V/I but remains active against the M204V single mutant in vitro, potentially explaining the difference in resistance profiles between telbivudine and lamivudine. ^[3]

プロトコル(参考用のみ)

参考

https://pubmed.ncbi.nlm.nih.gov/18474576/
https://pubmed.ncbi.nlm.nih.gov/20586931/
https://pubmed.ncbi.nlm.nih.gov/19028525/

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：

SARS-CoV-2 RdRp Inhibitors Selected from a Cell-Based SARS-CoV-2 RdRp Activity Assay System [ Biomedicines, 2021, 9(8)996]	PubMed: 34440200
Interferon alpha antagonizes the anti-hepatoma activity of the oncolytic virus M1 by stimulating anti-viral immunity. [ Oncotarget, 2017, 8(15):24694-24705]	PubMed: 28445966
MICE models: superior to the HERG model in predicting Torsade de Pointes. [Kramer J, et al. Sci Rep, 2013, 3:2105]	PubMed: 23812503

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。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。