SML3428

GLPG2938

≥97% (HPLC)

• Synonym(e): 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
• Empirische Formel (Hill-System): C₂₀H₁₉F₆N₇O₂
• CAS-Nummer: 2130996-00-6
• Molekulargewicht: 503.40
• UNSPSC Code: 12352200
• NACRES: NA.77
• MDL number: MFCD34563730
• Assay: ≥97% (HPLC)
• Form: powder

Eigenschaften

• Quality Segment: 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

Beschreibung

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.

Sicherheitshinweise

• Lagerklasse: 11 - Combustible Solids
• Was ist los?: WGK 3
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable