Vesatolimod (GS-9620)

製品コードS7221 バッチS722101

印刷

化学情報

Synonyms

Storage
(From the date of receipt)

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

化学式

C₂₂H₃₀N₆O₂

分子量

410.51

CAS No.

1228585-88-3

Solubility (25°C)*

体外

4-Methylpyridine (warmed with 50ºC water bath)

12 mg/mL (29.23 mM)

DMSO

8.8 mg/mL (21.43 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Clear solution

5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O

0.44mg/ml

Taking the 1 mL working solution as an example, add 50 μL of 8.8 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.

* <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	Vesatolimod (GS-9620) is a potent and selective orally active small molecule agonist of Toll-like receptor 7.
in vitro	GS-9620 potently inhibited viral replication in peripheral blood mononuclear cells(PBMCs), particularly when added 24 to 48 hours prior to HIV infection (EC50= 27 nM). Depletion of pDCs, but not other immune cell subsets from PBMC cultures, suppressed GS-9620 antiviral activity^[2].
in vivo	Short-term oral administration of GS-9620 provides long-term suppression of serum and liver HBV DNA. GS-9620 administration induces production of IFN-α and other cytokines and chemokines, and activates ISGs, natural killer cells, and lymphocyte subsets. Its treatment reduces viral DNA, Serum levels of HB surface antigen, HB e antigen and numbers of HBV antigen-positive hepatocytes while hepatocyte apoptosis increases^[1]. Currently, GS-9620 is under clinical evaluation for treating chronic HBV infection and for reducing latent reservoirs in virally-suppressed HIV-infected patients^[2].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	Human PBMCs
	濃度	serial dilutions
	反応時間	5 days
	実験の流れ	Uninfected PBMCs from individual donors are first activated in bulk using PHA and IL-2 at 37°C for 48 hours and then seeded into 96-well plates at a density of 2 x 10⁵ cells per well before being dosed in triplicate with 4-fold serial dilutions of compounds prepared in RPMI cell culture medium. Cells are incubated in a 5% CO2 incubator at 37°C for a period of 5 days. At the end of the assay, cell viability is assessed.
動物実験	動物モデル	chimpanzees
	投薬量	1 mg/kg and 2 mg/kg
	投与方法	oral administration

参考

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：

β-catenin regulates HIV latency and modulates HIV reactivation [ PLoS Pathog, 2022, 18(3):e1010354]	PubMed: 35255110
Determination of motolimod concentration in rat plasma by liquid chromatography-tandem mass spectrometry and its application in a pharmacokinetic study. [ J Pharm Biomed Anal, 2020, 179:112987]	PubMed: 31761376
Activation of type I interferon antiviral response in human neural stem cells. [ Stem Cell Res Ther, 2019, 10(1):387]	PubMed: 31843025
TLR7/8-agonist-loaded Nanoparticles Promote the Polarization of Tumour-Associated Macrophages to Enhance Cancer Immunotherapy [ Nat Biomed Eng, 2018, 2(8):578-588]	PubMed: 31015631
3D microfluidic liver cultures as a physiological preclinical tool for hepatitis B virus infection. [ Nat Commun, 2018, 9(1):682]	PubMed: 29445209
Structural Analyses of Toll-like Receptor 7 Reveal Detailed RNA Sequence Specificity and Recognition Mechanism of Agonistic Ligands. [ Cell Rep, 2018, 25(12):3371-3381]	PubMed: 30566863

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。