Tenofovir Alafenamide

製品コードS7856 バッチS785604

印刷

化学情報

Synonyms

GS-1278

Storage
(From the date of receipt)

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

化学式

C₂₁H₂₉N₆O₅P

分子量

476.47

CAS No.

379270-37-8

Solubility (25°C)*

体外

DMSO

95 mg/mL (199.38 mM)

Ethanol

95 mg/mL (199.38 mM)

Water

Insoluble

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.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	4.750mg/ml (9.97mM)	Taking the 1 mL working solution as an example, add 50 μL of 95 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	0.790mg/ml (1.66mM)	Taking the 1 mL working solution as an example, add 50 μL of 15.8 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <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	Tenofovir Alafenamideは、HIVおよびB型肝炎の治療に使用される逆転写酵素阻害剤であるテノホビルのプロドラッグです。
in vitro	GS-7340 has a potent anti-HIV activity with IC50 of 0.005 μM. GS 7340 has a half-life of 90 min in human plasma and a half-life of 28.3 min in an MT-2 cell extract at 37°C. the hepatic uptake of GS-7340 isfacilitated by OATP1B1 and OATP1B3, respectively. GS-7340 inhibits HBV reverse transcriptase after being converted to the pharmacologically active form, TFV-DP.
in vivo	In male beagle dogs, GS 7340 (10 mg/kg, p.o.) results in an enhanced distribution to lymphatic tissue.

プロトコル(参考用のみ)

動物実験	動物モデル	Male beagle dogs
	投薬量	10 mg/kg
	投与方法	p.o.

参考

https://pubmed.ncbi.nlm.nih.gov/11562962/
https://pubmed.ncbi.nlm.nih.gov/15855512/
https://pubmed.ncbi.nlm.nih.gov/25870059/

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：

Preclinical and clinical antiviral characterization of AB-836, a potent capsid assembly modulator against hepatitis B virus [ Antiviral Res, 2024, 231:106010]	PubMed: 39326502
Nucleos(t)ide analogs for hepatitis B virus infection differentially regulate the growth factor signaling in hepatocytes [ Hepatol Commun, 2024, 8(1)e0351]	PubMed: 38180972
In Vitro Susceptibility of HIV Isolates with High Growth Capability to Antiretroviral Drugs [ Int J Mol Sci, 2022, 23(23)15380]	PubMed: 36499705
Preclinical characterization of AB-506, an inhibitor of HBV replication targeting the viral core protein [ Antiviral Res, 2021, 197:105211]	PubMed: 34826506
Tenofovir Prodrugs Potently Inhibit Epstein-Barr Virus Lytic DNA Replication by Targeting the Viral DNA Polymerase [ Proc Natl Acad Sci U S A, 2020, 14;202002392]	PubMed: 32409608
Impact of vaginal microbiome communities on HIV antiretroviral-based pre-exposure prophylaxis (PrEP) drug metabolism [ PLoS Pathog, 2020, 16(12):e1009024]	PubMed: 33270801
Altered Gut Microbiome under Antiretroviral Therapy: Impact of Efavirenz and Zidovudine [ ACS Infect Dis, 2020, 10.1021/acsinfecdis.0c00536]	PubMed: 33346662
HIV-1 Subtype C with PYxE Insertion Has Enhanced Binding of Gag-p6 to Host Cell Protein ALIX and Increased Replication Fitness. [ J Virol, 2019, 93(9)]	PubMed: 30760577
Antiretroviral potency of 4'-ethnyl-2'-fluoro-2'-deoxyadenosine, tenofovir alafenamide and second-generation NNRTIs across diverse HIV-1 subtypes. [ J Antimicrob Chemother, 2018, 73(10):2721-2728]	PubMed: 30053052
How to Control HTLV-1-Associated Diseases: Preventing de Novo Cellular Infection Using Antiviral Therapy. [ Front Microbiol, 2018, 9:278]	PubMed: 29593659

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。