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1-[2-Ethoxy-6-(trifluoromethyl)-4-pyridyl]-3-[[5-methyl-6-[1-methyl-3-(trifluoromethyl)pyrazol-4-yl]pyridazin-3-yl]methyl]urea, GLPG 2938, GLPG-2938, N-[2-Ethoxy-6-(trifluoromethyl)-4-pyridinyl]-N′-[[5-methyl-6-[1-methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl]-3-pyridazinyl]methyl]urea
C20H19F6N7O2
Recommended Products
Quality Level
Assay
≥97% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
-10 to -25°C
SMILES string
O=C(NCC1=CC(C)=C(C2=CN(C)N=C2C(F)(F)F)N=N1)NC3=CC(C(F)(F)F)=NC(OCC)=C3
Biochem/physiol Actions
GLPG2938 is an orally active, potent 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 (1, 3, and 10 mg/kg b.i.d. p.o.) with good pharmacokinetics.
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Regulatory Information
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