T0070907

製品コードS2871 バッチS287104

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C12H8ClN3O3
分子量 277.66 CAS No. 313516-66-4
Solubility (25°C)* 体外 DMSO 55 mg/mL (198.08 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.
* <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 T0070907 is a potent inhibitor of PPARγ (peroxisome proliferator activator receptor γ ) that induces G2/M arrest and enhances the effect of radiation in human cervical cancer cells through mitotic catastrophe. It also acts as an antagonist of PPARγ that suppresses breast cancer cell proliferation and motility via both PPARgamma-dependent and -independent mechanisms.
in vitro

T0070907 is a potent and selective PPARγ antagonist. With an apparent binding affinity of 1 nM, this compound covalently modifies PPARγ on cysteine 313 in helix 3 of human PPARγ2. It blocks PPARγ function in both cell-based reporter gene and adipocyte differentiation assays. Consistent with its role as an antagonist of PPARγ, this chemical blocks agonist-induced recruitment of coactivator-derived peptides to PPARγ in a homogeneous time-resolved fluorescence-based assay and promotes recruitment of the transcriptional corepressor NCoR to PPARγ in both glutathione S-transferase pull-down assays and a PPARγ/retinoid X receptor (RXR) α-dependent gel shift assay. Studies with mutant receptors suggest that it modulates the interaction of PPARγ with these cofactor proteins by affecting the conformation of helix 12 of the PPARγ ligand-binding domain. Interestingly, whereas the T0070907-induced NCoR recruitment to PPARγ/RXRα heterodimer can be almost completely reversed by the simultaneous treatment with RXRα agonist LGD1069, this compound treatment has only modest effects on LGD1069-induced coactivator recruitment to the PPARγ/RXRα heterodimer. [1] This chemical treatment inhibits proliferation, invasion and migration but does not significantly affect apoptosis. Molecular inhibition using a dominant negative (Δ462) receptor yields similar results. It also mediates a dose-dependent decrease in phosphorylation of PPARγ, and its ability to bind to DNA, and may directly affect mitogen-activated protein kinase signaling. [2]
in vivo

Lipopolysaccharide preconditioning significantly attenuates the development of renal dysfunction, hepatocellular injury, and circulatory failure as well as the increase in the plasma levels of interleukin-1 [beta] caused by severe endotoxemia. This compound can attenuate all of these beneficial effects afforded by preconditioning with lipopolysaccharide [3]

プロトコル(参考用のみ)

キナーゼアッセイ Ligand Binding Assay
To determine the binding affinity of T0070907 to the PPARs, scintillation proximity assay (SPA) is performed with the following modifications. A 90-μl reaction contains SPA buffer (10 mm KH2PO4, 10 mm KH2PO4, 2 mm EDTA, 50 mm NaCl, 1 mm dithiothreitol, 2 mmCHAPS, 10% (v/v) glycerol, pH 7.1), 50 ng of GST-PPARγ (or 150 ng of GST-PPARα, GST-PPARδ), 5 nm 3H-labeled radioligands, and 5 μl of this compound in Me2SO. After incubation for 1 h at room temperature, 10 μl of polylysine-coated SPA beads (at 20 mg/ml in SPA buffer) are added, and the mixtureis incubated for 1 h before reading in Packard Topcount.
細胞アッセイ 細胞株 MCF-7 cells
濃度 20 μM and higher concentrations
反応時間 48 h
実験の流れ

MTS assay
動物実験 動物モデル Preconditioning is performed by administering a low dose (1 mg/kg) of Escherichia coli LPS (serotype 0.127:B8) intraperitoneally 24 hr before the induction of severe endotoxemia.
投薬量 1 mg/kg
投与方法 intraperitoneally

参考

  • https://pubmed.ncbi.nlm.nih.gov/11877444/
  • https://pubmed.ncbi.nlm.nih.gov/21498701/
  • https://pubmed.ncbi.nlm.nih.gov/16484917/
  • https://pubmed.ncbi.nlm.nih.gov/24642720/

カスタマーフィードバック

Data from [Data independently produced by , , Aging Cell, 2018, doi: 10.1111/acel.12774]

Data from [Data independently produced by , , Int Immunopharmacol, 2015, 26(1): 58-64]

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：

Gut symbiont-derived ursodeoxycholic acid promotes fatty acid oxidation to protect against renal ischemia-reperfusion injury [ Cell Rep Med, 2025, 6(10):102373] PubMed: 41015035
Stromal vascular fraction inhibits renal fibrosis by regulating metabolism and inflammation in obstructive nephropathy [ Front Pharmacol, 2025, 16:1559446] PubMed: 40432888
Diverse Lenabasum pathway activation in dermatomyositis patients' blood [ Sci Rep, 2025, 15(1):17232] PubMed: 40383862
Dysregulation of adipocytokines via the hsa-miR-548ay-3p/PPARγ signaling pathway leads to cardiac fibrosis [ Sci Rep, 2025, 15(1):27779] PubMed: 40739110
Interleukin-34-orchestrated tumor-associated macrophage reprogramming is required for tumor immune escape driven by p53 inactivation [ Immunity, 2024, 57(10):2344-2361.e7] PubMed: 39321806
Pro-ferroptotic signaling promotes arterial aging via vascular smooth muscle cell senescence [ Nat Commun, 2024, 15(1):1429] PubMed: 38365899
Targeted knockdown of PGAM5 in synovial macrophages efficiently alleviates osteoarthritis [ Bone Res, 2024, 12(1):15] PubMed: 38433252
Effect of genistein supplementation on microenvironment regulation of breast tumors in obese mice [ Breast Cancer Res, 2024, 26(1):147] PubMed: 39456028
Human TH9 cells rely on PPAR-γ-mediated cystine uptake to prevent lipid peroxidation and bioenergetic failure [ J Invest Dermatol, 2024, S0022-202X(24)03027-6] PubMed: 39725162
Anti-tumor effects of telmisartan in glioma-astrocyte non-contact co-cultures: A critical role of astrocytic IL-6-mediated paracrine growth promotion [ Int Immunopharmacol, 2024, 139:112707] PubMed: 39032472

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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