| Identification | Back Directory | [Name]
GLPG2938 | [CAS]
2130996-00-6 | [Synonyms]
GLPG2938 1-(2-Ethoxy-6-(trifluoromethyl)pyridin-4-yl)-3-((5-methyl-6-(1-methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl)pyridazin-3-yl)methyl)urea GLPG2938,GLPG 2938,Lysophospholipid Receptor,fibrosis,inhibit,LPL Receptor,GLPG-2938,selective,pulmonary,Inhibitor,potent,idiopathic | [Molecular Formula]
C20H19F6N7O2 | [MDL Number]
MFCD34563730 | [MOL File]
2130996-00-6.mol | [Molecular Weight]
503.4 |
| Chemical Properties | Back Directory | [Boiling point ]
585.9±50.0 °C(Predicted) | [density ]
1.49±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMF:10.0(Max Conc. mg/mL);19.86(Max Conc. mM) DMSO:51.5(Max Conc. mg/mL);102.3(Max Conc. mM) Ethanol:1.0(Max Conc. mg/mL);1.99(Max Conc. mM) | [form ]
A solid | [pka]
11.73±0.46(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
GLPG2938 is a potent and selective S1P2 antagonist. GLPG2938 can be used for the research of idiopathic pulmonary fibrosis[1]. | [Biological Activity]
GLPG2938 is an orally activepotent and selective S1P2 receptor (S1PR2) antagonist (GTPγS induction IC50 = 29 nM; [S1P] = EC80) with no activity against other S1P receptors. GLPG2938 inhibits sphingosine 1-phosphate (S1P)-induced cellular responses in cultures (Ca2+ flux IC50 = 8.8 nM & IL8 release IC50 = 3.8 nM; [S1P] = EC80) and exhibits good efficacy in a 14-day model of bleomycin-induced pulmonary fibrosis in mice in vivo (13and 10 mg/kg b.i.d. p.o.) with good pharmacokinetics. | [in vivo]
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.
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| [IC 50]
S1PR2 | [References]
[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. DOI:10.1021/acs.jmedchem.1c00138 |
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| Company Name: |
InvivoChem
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| Tel: |
13549236410 |
| Website: |
https://www.invivochem.cn/ |
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