An S1P2 antagonist
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GLPG2938

Item No. 34318

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[2-ethoxy-6-(trifluoromethyl)-4-pyridinyl]-N′-[[5-methyl-6-[1-methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl]-3-pyridazinyl]methyl]-urea
CAS Number
2130996-00-6
Molecular Formula
C20H19F6N7O2
Formula Weight
503.4
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMSO: 3 mg/mlEthanol: 1 mg/mlPBS (pH 7.2): insol
λmax
217 nm
SMILES
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
InChi Code
InChI=1S/C20H19F6N7O2/c1-4-35-15-7-11(6-14(29-15)19(21,22)23)28-18(34)27-8-12-5-10(2)16(31-30-12)13-9-33(3)32-17(13)20(24,25)26/h5-7,9H,4,8H2,1-3H3,(H2,27,28,29,34)
InChi Key
MGJMUVKYINFAQC-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    5 mg

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    10 mg

    $525

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    25 mg

    $1,062

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    Product Description

    GLPG2938 is sphingosine-1-phosphate receptor 2 (S1P2) antagonist.1 It inhibits S1P-induced calcium flux in CHO cells overexpressing human S1P2 (IC50 = 8.8 nM). GLPG2938 inhibits S1P-induced IL-8 release in HFL1 cells (IC50 = 0.6 nM) and S1P-induced contraction of human lung fibroblasts. In vivo, GLPG2938 (3, 10, and 30 mg/kg) prevents epithelial damage and pulmonary fibrosis, structural distortion, and inflammation in a mouse model of bleomycin-induced pulmonary fibrosis.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Mammoliti, O., Palisse, A., Joannesse, C., 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. 64(9), 6037-6058 (2021).