Resatorvid (TAK-242)

製品コードS7455 バッチS745503

印刷

化学情報

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

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	1%DMSO 1 40%PEG300 2 5%TWEEN80 3 54%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。	0.600mg/ml (1.66mM)	Taking the 1 mL working solution as an example, add 10 μL of 60 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 540 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	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	By binding directly to Cys747 in the intracellular TLR4 domain, Resatorvid (TAK-242) inhibits the TLR4 pathway. It disrupts the interactions of TLR4 with its adaptor molecules, TIRAP and TRAM^[1].
in vivo	Resatorvid (TAK-242) protects against acute cerebral ischemia/reperfusion injury in mice by dose of 3 mg/kg^[1]. Topical application of this compound can block UV-induced AP-1 activation in mouse epidermis. In a UV-induced skin tumorigenesis model, it 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]. It 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 (TAK-242) or vehicle and harvested 6 hr later. It 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

参考

https://pubmed.ncbi.nlm.nih.gov/28976923/
https://pubmed.ncbi.nlm.nih.gov/29437671/
https://pubmed.ncbi.nlm.nih.gov/23193438/

https://www.ncbi.nlm.nih.gov/pubmed/?term=27859308
https://pubmed.ncbi.nlm.nih.gov/16279805/

+ 展开

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：

Macrophages form dendrite-like pseudopods to enhance bacterial ingestion [ EMBO J, 2025, 10.1038/s44318-025-00515-z]	PubMed: 40721684
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α-Synuclein orchestrates Th17 responses as antigen and adjuvant in Parkinson's disease [ J Neuroinflammation, 2025, 22(1):38]	PubMed: 39934862
Cycloastragenol reduces inflammation in CLP-induced septic MICE by suppressing TLR4 signaling pathways [ Phytomedicine, 2025, 142:156645]	PubMed: 40319834
Sodium butyrate attenuates experimental neonatal necrotizing enterocolitis by suppressing TLR4-mediated NLRP3 inflammasome-dependent pyroptosis [ Food Funct, 2025, 16(9):3508-3524]	PubMed: 40223745
Mitochondrial ROS-ER Stress Axis Governs IL-10 Production in Neutrophils and Regulates Inflammation in Murine Chlamydia pneumoniae Lung Infection [ Cells, 2025, 14(19)1523]	PubMed: 41090752
Intracellular CIRP promotes liver regeneration via STAT3 signaling pathway activation after partial hepatectomy in mice [ Int J Mol Med, 2025, 55(3)42]	PubMed: 39791211
Bone Marrow Myeloid-Lymphatic Progenitors Expand Tumor Lymphatic Vasculature Through Cell Fusion [ Cancers (Basel), 2025, 17(11)1804]	PubMed: 40507286
GATA1 Transcriptionally Upregulates LMCD1, Promoting Ferroptosis in Sepsis-Associated Acute Kidney Injury Through the Hippo/YAP Pathway [ Kaohsiung J Med Sci, 2025, e70071.]	PubMed: 40650665
Identification of hypoxic macrophages in glioblastoma with therapeutic potential for vasculature normalization [ Cancer Cell, 2024, S1535-6108(24)00119-3]	PubMed: 38640932

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。