Olitigaltin (TD-139)

製品コードS0471 バッチS047104

印刷

化学情報

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

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	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%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。	5.000mg/ml (7.71mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 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 make it clear; then continue to add 500 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	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), a novel high-affinity inhibitor of the galectin-3 carbohydrate binding domain, reduces TGF-β1- induced β-catenin translocation to the nucleus and also blocks TGF-β1–induced β-catenin phosphorylation.^[2]
in vivo	A highly potent, selective inhibitor of Galectin-3 (Gal-3) carbohydrate, Olitigaltin (TD-139) 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 Olitigaltin (TD-139). Cells are lysed and analyzed for active β-catenin, total β-catenin, and β-actin by Western blot. After fixation, they are analyzed by immunofluorescence staining for active β-catenin (green) with nuclei stained using 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

参考

https://pubmed.ncbi.nlm.nih.gov/28166391/
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3410728/
https://pubmed.ncbi.nlm.nih.gov/22095546/

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：

Uptake of small extracellular vesicles by recipient cells is facilitated by paracrine adhesion signaling [ Nat Commun, 2025, 16(1):2419]	PubMed: 40075063
Rescue of mitochondrial dysfunction through alteration of extracellular matrix composition in barth syndrome cardiac fibroblasts [ Biomaterials, 2025, 315:122922]	PubMed: 39509858
Citrus pectin-coated inhalable PLGA nanoparticles for treatment of pulmonary fibrosis [ J Mater Chem B, 2025, 13(10):3325-3339]	PubMed: 39918485
Exosomal Galectin-3 promotes peritoneal metastases in gastric adenocarcinoma via microenvironment alterations [ iScience, 2025, 28(1):111564]	PubMed: 39811647
Intravitreal injection of the Galectin-3 inhibitor TD139 provides neuroprotection in a rat model of ocular hypertensive glaucoma [ Mol Brain, 2024, 17(1):84]	PubMed: 39574161
In vitro and in vivo effects of Galectin-3 inhibitor TD139 on inflammation and ERK/JNK/p38 pathway in gestational diabetes mellitus [ Kaohsiung J Med Sci, 2024, 40(10):916-925]	PubMed: 39230472
In vitro and in vivo effects of Galectin-3 inhibitor TD139 on inflammation and ERK/JNK/p38 pathway in gestational diabetes mellitus [ Kaohsiung J Med Sci, 2024, 40(10):916-925]	PubMed: 39230472
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

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。