GLPG2938

GLPG2938 is a potent and selective S1P2 antagonist. GLPG2938 can be used for the research of idiopathic pulmonary fibrosis[1].

Research Areas >> Others

Signaling Pathways >> GPCR/G Protein >> LPL Receptor

S1PR2

GLPG2938 (0.5~5 μM; HPF cells) significantly prevents the S1P-mediated contraction at all tested concentrations[1].

GLPG2938 (1~10 mg/kg; p.o.) displays a marked protective effect at all dosed tested, resulting in statistically significant reduction of the Ashcroft score[1]. GLPG2938 shows good pharmacokinetics, with long half-life, low clearance, and good bioavailability in all species, especially in dogs[1]. Animal Model: Male C57BL/6 mice[1] Dosage: 1~10 mg/kg Administration: P.o. Result: Displayed a marked protective effect at all dosed tested, resulting in statistically significant reduction of the Ashcroft score. 

[1]. Mammoliti O, 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;64(9):6037-6058.