SR-717 lithium

製品コードS0853 バッチS085302

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

C15H8F2LiN5O3

分子量 351.19 CAS No. 2375421-09-1
Solubility (25°C)* 体外 DMSO (warmed with 50ºC water bath) 35 mg/mL (99.66 mM)
Water Insoluble
Ethanol 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 10%Tween80 85%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。

3.000mg/ml (8.54mM) Taking the 1 mL working solution as an example, add 50 μL of 60 mg/ml clarified DMSO stock solution to 100 μL of Tween80, mix evenly to clarify; then continue to add 850 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 SR-717 lithium is a non-nucleotide STING agonist that demonstrates broad interspecies and interallelic specificity with EC50 of 2.1 μM and 2.2 μM in ISG-THP1 (WT) and ISG-THP1 (cGAS KO) cell lines, respectively. SR-717 lithium also induces the expression of clinically relevant targets, including programmed cell death 1 ligand 1 (PD-L1), in a STING-dependent manner. SR-717 lithium exhibits antitumor activity.
in vitro

SR-717 induces the expression of PD-L1 in THP1 cells and in primary human peripheral blood mononuclear cells in a STING-dependent manner.[1]

in vivo

SR-717 ( intraperitoneally for 7 days) displays antitumor activity in WT or Stinggt/gt mice; promots the activation of CD8+ T, natural killer, and dendritic cells in relevant tissues; and facilitates antigen cross-priming.

プロトコル(参考用のみ)

細胞アッセイ 細胞株 ISG-THP1 STING KO cell lines
濃度 3.8 μM
反応時間 4 h
実験の流れ

"Western blot analyses the impact of SR-717 delivery (3.8 mM) on PD-L1 expression in WT THP1 or ISG-THP1 STING KO (STING KO) cells."

動物実験 動物モデル Stinggt/gt mice
投薬量 30 mg/kg
投与方法 i.p.

参考

  • https://pubmed.ncbi.nlm.nih.gov/32820126/
  • https://pubmed.ncbi.nlm.nih.gov/32820126/

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:

Distinct oligomeric assemblies of STING induced by non-nucleotide agonists [ Nat Commun, 2025, 16(1):3440] PubMed: 40216780
Targeted Delivery of STING Agonist via Albumin Nanoreactor Boosts Immunotherapeutic Efficacy against Aggressive Cancers [ Pharmaceutics, 2024, 16(9)1216] PubMed: 39339252
Inhibition of cGAS in Paraventricular Nucleus Attenuates Hypertensive Heart Injury Via Regulating Microglial Autophagy [ Mol Neurobiol, 2022, 59(11):7006-7024] PubMed: 36070120
Inhibition of the cGAS-STING Pathway Attenuates Lung Ischemia/Reperfusion Injury via Regulating Endoplasmic Reticulum Stress in Alveolar Epithelial Type II Cells of Rats [ J Inflamm Res, 2022, 15:5103-5119] PubMed: 36091334
Sensing of cytoplasmic chromatin by cGAS activates innate immune response in SARS-CoV-2 infection [ Signal Transduct Target Ther, 2021, 6(1):382] PubMed: 34732709

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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