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SR-717
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
SR-717图片
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
SR-717 是一种非核苷酸 STING 激动剂,在 ISG-THP1 (WT) 和 ISG-THP1 cGAS KO (cGAS KO) 细胞系中的 EC50 分别为 2.1 μM 和 2.2 μM。

Cell lines

human umbilical vein endothelial cells (HUVECs)

Preparation Method

The cells were exposed to 2 μM SR-717 and challenged with 10% fetal bovine serum (FBS) for 2 h.

Reaction Conditions

2 μM SR-717 for two hours

Applications

Pharmacological targeting of cGAS/STING-YAP signaling by both a small-molecule STING agonist, SR-717 that blocks the profibrotic activity of endothelial YAP, attenuated liver and kidney fibrosis.

Animal models

Stinggt/gtmice

Preparation Method

The tumor growth was detected by intraperitoneal injection of SR-717 (30 mg/kg, once a day, for 1 week).

Dosage form

30 mg/kg SR-717 once-per-day for 1 week

Applications

SR-717 (30 mg/kg intraperitoneally for 7 days) displays antitumor activity; promots the activation of CD8+ T, natural killer, and dendritic cells in relevant tissues; and facilitates antigen cross-priming

产品描述

SR-717 is a stable cyclic guanosine monophosphate-adenosine monophosphate (cGAMP) mimetic, Antitumor activity[1]. The cGAS-STING pathway promotes the senescence of cancer cells, induces apoptosis of cancer cells, and increases the protective effect of cytotoxic T cells and natural killer cell-mediated cytotoxicity[4]. cGAS-STING pathway plays an important role in the chronic inflammatory status in various organs[5].SR-717 as a non-nucleotide STING agonist with EC50s of 2.1 μM and 2.2 μM in ISG-THP1 (WT) and ISG-THP1 cGAS KO (cGAS KO) cell lines, respectively.

Pharmacological targeting of cGAS/STING-YAP signaling by both a small-molecule STING agonist, SR-717 that blocks the profibrotic activity of endothelial YAP, attenuated liver and kidney fibrosis[2].

By STING agonist SR-717, activation of cGAS-STING pathway induced increased apoptosis, inflammation, and oxidative stress via regulating ERS and therefore resulted in pulmonary edema and pathological injury in the lungs of I/R rats[3].

References:
[1]: Chin EN, Yu C, et,al. Antitumor activity of a systemic STING-activating non-nucleotide cGAMP mimetic. Science. 2020 Aug 21;369(6506):993-999. doi: 10.1126/science.abb4255. PMID: 32820126.
[2]: Wang L, Zhang Y, et,al. Pharmacological targeting of cGAS/STING-YAP axis suppresses pathological angiogenesis and ameliorates organ fibrosis. Eur J Pharmacol. 2022 Sep 2;932:175241. doi: 10.1016/j.ejphar.2022.175241. Epub ahead of print. PMID: 36058291.
[3]: Huang R, Shi Q, et,al. 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 Sep 5;15:5103-5119. doi: 10.2147/JIR.S365970. PMID: 36091334; PMCID: PMC9462969.
[4]: Du H, Xu T, et,al. cGAS-STING signaling in cancer immunity and immunotherapy. Biomed Pharmacother. 2021 Jan;133:110972. doi: 10.1016/j.biopha.2020.110972. Epub 2020 Nov 27. PMID: 33254021.
[5]: Bao T, Liu J, et,al. The cGAS-STING pathway: more than fighting against viruses and cancer. Cell Biosci. 2021 Dec 14;11(1):209. doi: 10.1186/s13578-021-00724-z. PMID: 34906241; PMCID: PMC8670263.