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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.
Orally active, potent and selective S1P2 subtype-selective sphingosine-1-phosphate (S1P) receptor antagonist with in vitro and in vivo efficacy.
| Quality Level | 100 |
| 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 |
| 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 |
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¥ 521.16
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¥ 3683.17
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¥ 3317.36
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¥ 1153.44
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¥ 1361.98
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¥ 981.17
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¥ 839.71
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