Olitigaltin (TD-139)

製品コードS0471 バッチS047102

印刷

化学情報

Chemical Structure Synonyms GB0-139 Storage
(From the date of receipt)		 3 years -20°C powder
化学式

C28H30F2N6O8S
分子量 648.64 CAS No. 1450824-22-2
Solubility (25°C)* 体外 DMSO 100 mg/mL (154.16 mM)
Water Insoluble
Ethanol 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 Olitigaltin (TD-139, GB0-139) is a potent and selective inhibitor of galectin-3 with Kd of 0.036 µM over galectin-1 and galectin-7 with Kd of 2.2 µM and 32 µM, respectively. TD-139 is used potentially for the treatment of idiopathic pulmonary fibrosis (IPF).
in vitro

In primary lung alveolar epithelial cells (AECs), Olitigaltin (TD-139) which is a novel high-affinity inhibitor of the galectin-3 carbohydrate binding domain, reduces TGF-β1- induced β-catenin translocation to the nucleus, also blocks TGF-β1–induced β-catenin phosphorylation.[2]
in vivo

Olitigaltin (TD-139), a highly potent, selecitve inhibitor of Galectin-3 (Gal-3) carbohydrate, produces a significant decrease in total lung collagen, also decreases β-catenin activation in bleomycin model of pulmonary fibrosis.[2]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 primary alveolar epithelial cells from wild-type (WT) mice
濃度 10 μM
反応時間
実験の流れ

Primary alveolar epithelial cells from wild-type (WT) mice are plated and treated with transforming growth factor (TGF)-β1 in the presence or absence of 10 μM TD139. Cells are lysed and analyzed for active β-catenin, total β-catenin, and β-actin by Western blot. Cells are fixed and analyzed by immunofluorescence staining for active β-catenin (green) nuclei stained with DAPI (scale bar = 15 μm).
動物実験 動物モデル C57/Bl6 mice models of lung fibrosis
投薬量 10 µg
投与方法 instilled into the lungs

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：

Vdelta1 T cells are more resistant than Vdelta2 T cells to the immunosuppressive properties of galectin-3 [ Front Immunol, 2023, 14:1286097] PubMed: 38259448
Epithelial Galectin-3 Induced the Mitochondrial Complex Inhibition and Cell Cycle Arrest of CD8+ T Cells in Severe/Critical COVID-19 [ Int J Mol Sci, 2023, 24(16)12780] PubMed: 37628961
Epithelial Galectin-3 Induced the Mitochondrial Complex Inhibition and Cell Cycle Arrest of CD8+ T Cells in Severe/Critical COVID-19 [ Int J Mol Sci, 2023, 24(16)12780] PubMed: 37628961
Inhibition of Galectin-3 in a Rat Model of Epilepsy and Kainate-Activated BV2 Cells Limits Microglial Activation Through the NLRP3/Pyroptosis Pathway [ Neuroimmunomodulation, 2023, 30(1):325-337] PubMed: 37926077
Galectin-3 promotes the adipogenic differentiation of PDGFRα+ cells and ectopic fat formation in regenerating muscle [ Development, 2022, dev.199443] PubMed: 35029658
Ataxia telangiectasia and Rad3-related inhibition by AZD6738 enhances gemcitabine-induced cytotoxic effects in bladder cancer cells [ Front Allergy, 2022, 3:840454] PubMed: 35386657

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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