Resatorvid (TAK-242)

製品コードS7455 バッチS745501

印刷

化学情報

Chemical Structure Synonyms CLI-095 Storage
(From the date of receipt)		 3 years -20°C powder
化学式

C15H17ClFNO4S
分子量 361.82 CAS No. 243984-11-4
Solubility (25°C)* 体外 DMSO 72 mg/mL (198.99 mM)
Ethanol 72 mg/mL (198.99 mM)
Water Insoluble
* <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 Resatorvid (TAK-242, CLI-095) is a small-molecule-specific inhibitor of Toll-like receptor (TLR) 4 signaling, blocking LPS-induced production of NO, TNF-α and IL-6 in macrophages with IC50 of 1.8 nM, 1.9 nM and 1.3 nM, respectively. Resatorvid downregulates expression of TLR4 downstream signaling molecules MyD88 and TRIF. Resatorvid inhibits autophagy.
in vitro

TAK-242 inhibits the TLR4 pathway by binding directly to a Cys747 in the intracellular TLR4 domain. TAK-242 disrupts the interactions of TLR4 with its adaptor molecules, TIRAP and TRAM[1].
in vivo

TAK-242 protects against acute cerebral ischemia/reperfusion injury in mice by dose of 3 mg/kg[1]. Topical resatorvid can block UV-induced AP-1 activation in mouse epidermis. In a UV-induced skin tumorigenesis model, topical resatorvid displays potent photochemopreventive activity, significantly suppressing tumor area and multiplicity. Tumors harvested from resatorvid-treated mice display reduced activity of UV-associated signaling pathways and a corresponding increase in apoptosis compared to tumors from control animals[2]. TAK-242 significantly reduces the neuronal damage occurring after cerebral ischemia, a form of stroke in mice[3].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 Primary human keratinocytes
濃度 10 µM
反応時間 6 h
実験の流れ

NF-κB keratinocytes are treated with UVB +/− 10 µM resatorvid (or vehicle) and harvested 6 hr later. Resatorvid significantly inhibits UV-induced NF-κB luciferase signaling in keratinocytes.
動物実験 動物モデル male ddY mice aged 4-5weeks
投薬量 1 μl (at 0.001, 0.03, or 0.01 μg/μl)
投与方法 intracerebroventricularly

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：

Macrophage Tim-3 maintains intestinal homeostasis in DSS-induced colitis by suppressing neutrophil necroptosis [ Redox Biol, 2024, 70:103072] PubMed: 38330550
Fusobacterium nucleatum-triggered neutrophil extracellular traps facilitate colorectal carcinoma progression [ J Exp Clin Cancer Res, 2023, 42(1):236] PubMed: 37684625
Fusobacterium nucleatum-triggered neutrophil extracellular traps facilitate colorectal carcinoma progression [ J Exp Clin Cancer Res, 2023, 42(1):236] PubMed: 37684625
The PTX3/TLR4 autocrine loop as a novel therapeutic target in triple negative breast cancer [ Exp Hematol Oncol, 2023, 12(1):82] PubMed: 37749607
Dual RNA-Sequencing and Liquid Chromatography-Mass Spectrometry Unveil Specific Insights on the Pathogenicity of Trichophyton mentagrophytes Complex [ J Invest Dermatol, 2023, 143(3):470-479.e6] PubMed: 38295003
Extracellular vesicles produced by avian pathogenic Escherichia coli (APEC) activate macrophage proinflammatory response and neutrophil extracellular trap (NET) formation through TLR4 signaling [ Microb Cell Fact, 2023, 22(1):177.] PubMed: 37689682
Extracellular vesicles produced by avian pathogenic Escherichia coli -APEC) activate macrophage proinflammatory response and neutrophil extracellular trap -NET) formation through TLR4 signaling [ Microb Cell Fact, 2023, 22(1):177] PubMed: 37689682
Extracellular vesicles produced by avian pathogenic Escherichia coli (APEC) activate macrophage proinflammatory response and neutrophil extracellular trap (NET) formation through TLR4 signaling [ Microb Cell Fact, 2023, 22(1):177] PubMed: 37689682
Adh Promotes Actinobacillus pleuropneumoniae Survival in Porcine Alveolar Macrophages by Inhibiting CHAC2-Mediated Respiratory Burst and Inflammatory Cytokine Expression [ Cells, 2023, 12(5)696] PubMed: 36899832
Autophagy Activation in Peripheral Blood Mononuclear Cells of Peritoneal Dialysis Patients [ Kidney Int Rep, 2023, 8(9):1852-1863] PubMed: 37705917

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。