H-151

製品コードS6652 バッチS665204

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

C17H17N3O

分子量 279.34 CAS No. 941987-60-6
Solubility (25°C)* 体外 DMSO 56 mg/mL (200.47 mM)
Ethanol 14 mg/mL (50.11 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 40%PEG300 5%Tween80 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。

4.000mg/ml (14.32mM) Taking the 1 mL working solution as an example, add 50 μL of 80 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 H-151 is a highly potent and covalent antagonist of STING that has noteworthy inhibitory activity both in human cells and in vivo.
in vivo

After intraperitoneal administration, H-151 reachs effective systemic levels, displays a short half-life in the serum and formed an adduct to mmSTING. Notably, pretreatment of this compound markedly reduces systemic cytokine responses in CMA-treated mice. Moreover, it exhibits notable efficacy in Trex1−/− mice that expressed a bioluminescent IFNβ reporter, when administered for one week.[1]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 FLDMs
濃度 25 µM
反応時間 12 h
実験の流れ

Cells were treated with indicated concentrations of this compound.

動物実験 動物モデル C57BL/6J mice
投薬量 750 nM
投与方法 i.p.

参考

  • https://www.ncbi.nlm.nih.gov/pubmed/?term=Targeting+STING+with+covalent+small-molecule+inhibitors
  • https://pubmed.ncbi.nlm.nih.gov/36198273/

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:

Irisin-mediated muscle-renal crosstalk as a protective mechanism against contrast-induced acute kidney injury via cGAS-STING signalling inhibition [ Clin Transl Med, 2025, 15(3):e70235] PubMed: 40008481
TDP43 augments astrocyte inflammatory activity through mtDNA-cGAS-STING axis in NMOSD [ J Neuroinflammation, 2025, 22(1):14] PubMed: 39844196
CAD hijacks STING to impair antitumor immunity and radiotherapy efficacy of colorectal cancer [ Cell Death Dis, 2025, 16(1):641] PubMed: 40849416
Development of a TBK1 and ALK dual inhibitor for alleviating depressive behavior via anti-inflammatory effects [ Biomed Pharmacother, 2025, 186:117991] PubMed: 40117902
EZH2 inhibits senescence-associated inflammation and attenuates intervertebral disc degeneration by regulating the cGAS/STING pathway via H3K27me3 [ Osteoarthritis Cartilage, 2025, S1063-4584(25)00796-4] PubMed: 39938633
LAPTM5 exacerbates STING-mediated inflammation induced by LL-37 through stabilizing STING in rosacea [ Commun Biol, 2025, 8(1):1470] PubMed: 41087666
Profile of STING agonist and inhibitor research: a bibliometric analysis [ Front Pharmacol, 2025, 16:1528459] PubMed: 40008133
Brazilin Inhibits the Proliferation of Non-Small Cell Lung Cancer by Regulating the STING/TBK1/IRF3 Pathway [ J Cell Mol Med, 2025, 29(13):e70688] PubMed: 40596709
Ciprofloxacin enhances RSL3-induced ferroptosis by promoting mitochondrial Zn2+ accumulation via the STING1-CAV2 pathway [ J Biol Chem, 2025, 301(10):110653] PubMed: 40889676
STING orchestrates the neuronal inflammatory stress response in multiple sclerosis [ Cell, 2024, 187(15):4043-4060.e30.] PubMed: 38878778

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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