Emtricitabine (FTC)

製品コードS1704 バッチS170406

印刷

化学情報

Synonyms

BW 1592

Storage
(From the date of receipt)

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

化学式

C₈H₁₀FN₃O₃S

分子量

247.25

CAS No.

143491-57-0

Solubility (25°C)*

体外

Water

100 mg/mL (404.44 mM)

DMSO

49 mg/mL (198.17 mM)

Ethanol

49 mg/mL (198.17 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	エムトリシタビン（FTC）は、ヒト免疫不全ウイルス（HIV）とB型肝炎ウイルスの両方に活性を持つ新しいヌクレオシド系薬剤です。これはreverse transcriptase阻害剤です。細胞内半減期は39時間です。
in vitro	Emtricitabine (FTC) moderately reduces hepatocyte proliferation independent of effects on mtDNA in HepG2 human hepatoma cells, and when combined with tenofovir, slightly reduces cell proliferation without affecting mitochondrial parameters. It efficiently converts to its active metabolites in PBMCs and CEM cells, and displays additive to synergistic activity against HIV replication in PBMCs when combined with tenofovir, resulting in strongly synergistic anti-HIV activity in MT-2 cells against both wild-type and mutant virus. This compound demonstrates antiviral activity against laboratory adapted strains of HIV-1 and HIV-2 in various cell systems, and also exhibits antiviral activity in cell culture against feline and simian immuno-deficiency viruses (SIVs). It consistently shows up to 10-fold greater activity than lamivudine against all viruses tested in all T-cell lines, and generally demonstrates greater potency in vitro in human PBMCs than in MT-4 lines. Additionally, it exhibits anti-HBV activity in vitro (EC50, 0.01–0.04 µM) that is comparable to the anti-HBV activity of 3TC. It is approximately fourfold more active than 3TC in assays in the transformed T-cell line MT-4 infected with HIV-(1IIIB), whereas zidovudine is more active than this compound. Emtricitabine, lamivudine, and zidovudine are equally active against a panel of eight primary HIV-1 isolates from antiretroviral-naive subjects in PBMCs.

製品説明

エムトリシタビン（FTC）は、ヒト免疫不全ウイルス（HIV）とB型肝炎ウイルスの両方に活性を持つ新しいヌクレオシド系薬剤です。これはreverse transcriptase阻害剤です。細胞内半減期は39時間です。

in vitro

Emtricitabine (FTC) moderately reduces hepatocyte proliferation independent of effects on mtDNA in HepG2 human hepatoma cells, and when combined with tenofovir, slightly reduces cell proliferation without affecting mitochondrial parameters. It efficiently converts to its active metabolites in PBMCs and CEM cells, and displays additive to synergistic activity against HIV replication in PBMCs when combined with tenofovir, resulting in strongly synergistic anti-HIV activity in MT-2 cells against both wild-type and mutant virus. This compound demonstrates antiviral activity against laboratory adapted strains of HIV-1 and HIV-2 in various cell systems, and also exhibits antiviral activity in cell culture against feline and simian immuno-deficiency viruses (SIVs). It consistently shows up to 10-fold greater activity than lamivudine against all viruses tested in all T-cell lines, and generally demonstrates greater potency in vitro in human PBMCs than in MT-4 lines. Additionally, it exhibits anti-HBV activity in vitro (EC50, 0.01–0.04 µM) that is comparable to the anti-HBV activity of 3TC. It is approximately fourfold more active than 3TC in assays in the transformed T-cell line MT-4 infected with HIV-(1IIIB), whereas zidovudine is more active than this compound. Emtricitabine, lamivudine, and zidovudine are equally active against a panel of eight primary HIV-1 isolates from antiretroviral-naive subjects in PBMCs.

プロトコル(参考用のみ)

参考

https://pubmed.ncbi.nlm.nih.gov/18018766/
https://pubmed.ncbi.nlm.nih.gov/16759055/
https://pubmed.ncbi.nlm.nih.gov/11491420/

https://pubmed.ncbi.nlm.nih.gov/16323102/
https://pubmed.ncbi.nlm.nih.gov/12626884/

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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：

LINE-1 ORF1p Mimics Viral Innate Immune Evasion Mechanisms in Pancreatic Ductal Adenocarcinoma [ Cancer Discov, 2025, 10.1158/2159-8290.CD-24-1317]	PubMed: 39919290
In vitro and patient studies with platelets to explore off-target cardiovascular effects of integrase inhibitors [ HIV Med, 2025, 26(2):285-294]	PubMed: 39544128
Cognate antigen engagement induces HIV-1 expression in latently infected CD4+ T cells from people on long-term antiretroviral therapy [ Immunity, 2024, 57(12):2928-2944.e6]	PubMed: 39612916
Significance of hepatitis B virus capsid dephosphorylation via polymerase [ J Biomed Sci, 2024, 31(1):34]	PubMed: 38561844
IKAROS expression drives the aberrant metabolic phenotype of macrophages in chronic HIV infection [ Clin Immunol, 2024, 260:109915]	PubMed: 38286172
Dexrazoxane inhibits the growth of esophageal squamous cell carcinoma by attenuating SDCBP/MDA-9/syntenin-mediated EGFR-PI3K-Akt pathway activation [ Sci Rep, 2024, 14(1):9167]	PubMed: 38649770
Biological and Structural Analyses of New Potent Allosteric Inhibitors of HIV-1 Integrase [ Antimicrob Agents Chemother, 2023, 67(7):e0046223]	PubMed: 37310224
Acute antagonism in three-drug combinations for vaginal HIV prevention in humanized mice [ Sci Rep, 2023, 13(1):4594]	PubMed: 36944714
Reverse Transcriptase Inhibition Disrupts Repeat Element Life Cycle in Colorectal Cancer [ Cancer Discov, 2022, candisc.1117.2021]	PubMed: 35320348
Cell-to-cell transmission of HIV-1 from provirus-activated cells to resting naïve and memory human primary CD4 T cells is highly efficient and requires CD4 and F-actin but not chemokine receptors [ J Med Virol, 2022, 10.1002/jmv.28005]	PubMed: 35840493

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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