PF-00835231

製品コードS9731 バッチS973101

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
化学式

C24H32N4O6
分子量 472.53 CAS No. 870153-29-0
Solubility (25°C)* 体外 DMSO 95 mg/mL (201.04 mM)
Ethanol 95 mg/mL (201.04 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 95% Corn oil
0.59mg/ml Taking the 1 mL working solution as an example, add 50 μL of 11.8 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. 
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
4.75mg/ml 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. 
* <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 PF-00835231 is a 3CLpro (Mpro) inhibitor that may targets SARS-CoV-2 protease 3CLpro as a potential new treatment for COVID-19.
in vitro

A time-of-drug-addition approach delineates the timing of early SARS-CoV-2 life cycle steps in A549+ACE2 cells and validates PF-00835231's early time of action. In a model of the human polarized airway epithelium, PF-00835231 potently inhibits SARS-CoV-2 at low micromolar concentrations. PF-00835231 exhibits the potential as an effective SARS-CoV-2 antiviral.[1]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 A549 cells, human airway epithelial cultures (HAEC)
濃度 1 nM-10 μM
反応時間 0-4 h
実験の流れ

A549+ACE2 cells are seeded into black wall 96-well plates at 70% confluency. The next day, media is removed and replaced with complete media containing compound (PF-00835231)/carrier two hours prior to infection. Cells are then infected at 0.425 multiplicity of infection (MOI), based on Vero E6 titer, at 37°C. 1 hour post virus addition, virus is removed, and media containing compound/carrier is added. At 24 and 48 hours post infection, cells are fixed by submerging in 10% formalin solution for 30-45 min. After fixation, cells are washed once with H2O to remove excess formalin.

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：

Human NLRP1 is a sensor of pathogenic coronavirus 3CL proteases in lung epithelial cells [ Mol Cell, 2022, S1097-2765(22)00433-6] PubMed: 35594856
Identification of Aloe-derived natural products as prospective lead scaffolds for SARS-CoV-2 main protease (Mpro) inhibitors [ Bioorg Med Chem Lett, 2022, 66:128732] PubMed: 35427739
Design of modular autoproteolytic gene switches responsive to anti-coronavirus drug candidates [ Nat Commun, 2021, 12(1):6786] PubMed: 34811361
Pre-Steady-State Kinetics of the SARS-CoV-2 Main Protease as a Powerful Tool for Antiviral Drug Discovery [ Front Pharmacol, 2021, 12:773198] PubMed: 34938188

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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