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经验公式(希尔记法):
C20H19F6N7O2
化学文摘社编号:
分子量:
503.40
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
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
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
assay
≥97% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
-10 to -25°C
Quality Level
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.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
新产品
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