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2130996-00-6

2130996-00-6 Structure

2130996-00-6 Structure
IdentificationBack 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 PropertiesBack 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
Safety DataBack Directory
[Symbol(GHS) ]


GHS07
[Signal word ]

Warning
[Hazard statements ]

H302-H315-H319-H335
[Precautionary statements ]

P261-P264-P270-P271-P280-P301+P312-P302+P352-P304+P340-P305+P351+P338-P330-P332+P313-P337+P313-P362-P403+P233-P405-P501
Hazard InformationBack 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. ?
[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
Spectrum DetailBack Directory
[Spectrum Detail]

GLPG2938(2130996-00-6)1HNMR
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