|1-(2-乙氧基-6-(三氟甲基)吡啶-4-基)-3-((5-甲基-6-(1-甲基-3-(三氟甲基)-1H-吡唑-4-基)哒嗪-3-基)甲基)脲|CsnPharm

CAS No.: 2130996-00-6

GLPG2938 Catalog No. CSN28759

Synonyms: MUN-96006

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.

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靶点选择性

生物活性

实验方案

技术信息

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].
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.

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
- 1.9865 mL
- 9.9324 mL
- 19.8649 mL
- 5 mM
- 0.3973 mL
- 1.9865 mL
- 3.9730 mL
- 10 mM
- 0.1986 mL
- 0.9932 mL
- 1.9865 mL

技术信息

CAS号	2130996-00-6	储存条件	粉末 Sealed in dry,Room Temperature 液体 -20°C:3-6 月 -80°C:12月
分子式	C20H19F6N7O2	运输	蓝冰
分子量	503.40	别名	MUN-96006

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