GLPG2938 | S1P2 Antagonist | AmBeed-信号通路专用抑制剂

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GLPG2938 {[allProObj[0].p_purity_real_show]}

货号：A1473679

GLPG2938 is a pontent antagonist of S1P2 receptor, with exquisite potency on a phenotypic IL8 release assay, good pharmacokinetics, and good activity in a bleomycin-induced model of pulmonary fibrosis.

GLPG2938 化学结构
CAS号：2130996-00-6

GLPG2938 3D分子结构
CAS号：2130996-00-6

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GLPG2938 纯度/质量文件产品仅供科研

货号：A1473679 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • JACS Au, 2024. Ambeed. [ A148168 ]; • JMC, 2024. Ambeed. [ A187643 ]; • JMC, 2024. Ambeed. [ A341145 , A633512 , A607865 , A167774 ]; • Biomacromolecules, 2024. Ambeed. [ A110759 ]; • Biomacromolecules, 2024. Ambeed. [ A203543 ]; 更多 >

GLPG2938 生物活性

描述

Sphingosine 1-phosphate (S1P), a metabolic product of cell membrane sphingolipids, is bound to extracellular chaperones, is enriched in circulatory fluids, and binds to G protein-coupled S1P receptors (S1PRs) to regulate embryonic development, postnatal organ function, and disease. S1PRs regulate essential processes such as adaptive immune cell trafficking, vascular development, and homeostasis. Moreover, S1PR signaling is a driver of multiple diseases^[1]. S1P regulates cell fate, vascular tone, endothelial function and integrity as well as lymphocyte trafficking, thus disbalance in its production and signaling has been linked with development of such pathologies as arterial hypertension, atherosclerosis, endothelial dysfunction and aberrant angiogenesis. Number of signaling mechanisms are critical - from endothelial nitric oxide synthase through STAT3, MAPK and Akt pathways to HDL particles involved in redox and inflammatory balance^[2]. In vivo, HDL-S1P injection significantly reduced pulmonary oedema and endothelial leakage in septic rats. In vitro, cell experiments showed that HDL-S1P effectively protected the proliferation and migration abilities of endothelial cells, which could be partly explained by its biased activation of the S1P receptor 1^[3]. GLPG2938 is an antagonists of S1P receptor for prophylaxis and/or treatment of diseases including fibrotic, inflammatory, autoimmune, metabolic, cardiovascular, and/or proliferative diseases. GLPG2938 displayed S1P inhibitory activity with EC50 value of 9.5 nM (S1P2 antagonist EC50)^[4].

GLPG2938 参考文献

[1] Andreane Cartier,Timothy Hla. Sphingosine 1-phosphate: Lipid signaling in pathology and therapy. Science. 2019 Oct 18;366(6463):eaar5551.

[2]E Jozefczuk,et al. Significance of sphingosine-1-phosphate in cardiovascular physiology and pathology. Pharmacol Res. 2020 Jun;156:104793.

[3]YiWen Fan,et al. HDL-S1P protects endothelial function and reduces lung injury during sepsis in vivo and in vitro. Int J Biochem Cell Biol. 2020 Sep;126:105819.

[4]Oscar Mammoliti,et al. Discovery of the S1P2 Antagonist GLPG2938 (1-[2-Ethoxy-6-(trifluoromethyl)-4-pyridyl]-3-[[5-methyl-6-[1-methyl-3-(trifluoromethyl)pyrazol-4-yl]pyridazin-3-yl]methyl]urea), a Preclinical Candidate for the Treatment of Idiopathic Pulmonary Fibrosis. J Med Chem. 2021 May 13;64(9):6037-6058.

GLPG2938 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

1.99mL

0.40mL

0.20mL

9.93mL

1.99mL

0.99mL

19.86mL

3.97mL

1.99mL

GLPG2938 技术信息

CAS号	2130996-00-6
分子式	C₂₀H₁₉F₆N₇O₂
分子量	503.401

别名
运输	蓝冰

存储条件

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 105 mg/mL(208.58 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验配方

摩尔计算器

计算溶液所需的质量，体积或浓度。 Ambeed 摩尔浓度计算器基于以下方程式：

浓度 (mol/L) × 体积 (L) × 分子量 (g/mol)=质量 (g)

浓度

体积

分子量

质量

GLPG2938 {[allProObj[0].p_purity_real_show]}

GLPG2938 纯度/质量文件产品仅供科研

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GLPG2938 {[allProObj[0].p_purity_real_show]}

GLPG2938 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

GLPG2938 质控信息

GLPG2938 生物活性

GLPG2938 参考文献

GLPG2938 实验方案

GLPG2938 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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GLPG2938 纯度/质量文件产品仅供科研