|(2R,2'R,3R,3'R,4S,4'S,5R,5'R,6S,6'S)-6,6'-硫基双(4-(4-(3-氟苯基)-1H-1,2,3-三唑-1-基)-2-(羟甲基)四氢-2H-吡喃-3,5-二醇)|CsnPharm

CAS No.: 1450824-22-2

(2R,2'R,3R,3'R,4S,4'S,5R,5'R,6S,6'S)-6,6'-Thiobis(4-(4-(3-fluorophenyl)-1H-1,2,3-triazol-1-yl)-2-(hydroxymethyl)tetrahydro-2H-pyran-3,5-diol) Catalog No. CSN21130

Synonyms: GB0-139;半乳凝素-3抑制剂

TD139 is an inhibitor of the galectin-3 carbohydrate binding domain with Kd of 14 nM and shows therapeutic efficacy against idiopathic pulmonary fibrosis (IPF).

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400-920-2911

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实验方案

技术信息

生物活性

描述Galectins form a family of soluble lectins that take part in a wide range of biological processes, such as cell adhesion, cell migration, signaling, intracellular trafficking, cell proliferation, apoptosis, gene expression regulation, inflammation, and immune response. TD 139 is an effective and selective galectin-3 inhibitor with a K_d value of 0.036 µM and K_d values of 2.2 µM and 32 µM for galectin-1 and galectin-7, respectively. TD 139 can be used for the treatment of idiopathic pulmonary fibrosis (IPF)^[1]. In primary lung alveolar epithelial cells (AECs), TD 139 (10 µM) reduced TGF-β1–induced β-catenin translocation to the nucleus, with most of the β-catenin remaining at the cell surface. In the lungs of wild-type mice treated with 10 µg TD 139, there was marked reduction in fibrosis and β-catenin activation accompanied by decreased galectin-3 expression. TD 139 produced a significant decrease in total lung collagen^[2].
作用机制TD 139 interacts with the five binding subsites (A–E) that comprise the CRD (carbohydrate recognition domain) of galectin-3^[1].
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT02257177	Idiopathic Pulmonary Fibrosis	Phase 1 Phase 2	Completed	-	United Kingdom ... more >> Royal Devon & Exeter Foundation NHS Trust Exeter, Devon, United Kingdom, EX2 5DW Edinburgh University Hospital Edinburgh, Scotland, United Kingdom, EH16 4SA The Newcastle Upon Tyne Hospitals NHS Foundation Trust Newcastle, Tyne and Wear, United Kingdom, NE3 3HD Simbec Research Limited Merthyr Tydfil, Wales, United Kingdom, CF48 4DR Royal Brompton Hospital London, United Kingdom, SW3 6NP Collapse <<

参考文献

[1] Dion J, Deshayes F, Storozhylova N, et al. Lactosamine-Based Derivatives as Tools to Delineate the Biological Functions of Galectins: Application to Skin Tissue Repair. Chembiochem. 2017 Apr 18;18(8):782-789
[2] Mackinnon AC, Gibbons MA, Farnworth SL, et al. Regulation of transforming growth factor-β1-driven lung fibrosis by galectin-3. Am J Respir Crit Care Med. 2012 Mar 1;185(5):537-46

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.5417 mL
- 7.7085 mL
- 15.4170 mL
- 5 mM
- 0.3083 mL
- 1.5417 mL
- 3.0834 mL
- 10 mM
- 0.1542 mL
- 0.7708 mL
- 1.5417 mL

技术信息

CAS号

1450824-22-2

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C28H30F2N6O8S

运输

蓝冰

分子量

648.64

别名

GB0-139;半乳凝素-3抑制剂

溶解度

DMSO	180.0 mg/mL (277.5 mM)
Water	insoluble

动物实验配方

1% DMSO + water

0.1 mg/mL

clear

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(2R,2'R,3R,3'R,4S,4'S,5R,5'R,6S,6'S)-6,6'-Thiobis(4-(4-(3-fluorophenyl)-1H-1,2,3-triazol-1-yl)-2-(hydroxymethyl)tetrahydro-2H-pyran-3,5-diol) Catalog No. CSN21130

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