产品描述: | GLPG2938 是一种有效和选择性 S1P2 拮抗剂。GLPG2938 可用于特发性肺纤维化的研究。 |
靶点: |
S1PR2;S1PReceptor;LPLReceptor |
体外研究: |
GLPG2938 (0.5~5 μM; HPF cells) significantly prevents the S1P-mediated contraction at all tested concentrations. |
体内研究: |
GLPG2938 (1~10 mg/kg; p.o.) displays a marked protective effect at all dosed tested, resulting in statistically significant reduction of the Ashcroft score. GLPG2938 shows good pharmacokinetics, with long half-life, low clearance, and good bioavailability in all species, especially in dogs. |
参考文献: |
1.Mammoliti O, 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 Pulmona |
溶解性: |
Souble in DMSO |
保存条件: |
-20℃ |
配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
1 mM |
1.986 ml |
9.932 ml |
19.865 ml |
5 mM |
0.397 ml |
1.986 ml |
3.973 ml |
10 mM |
0.199 ml |
0.993 ml |
1.986 ml |
50 mM |
0.04 ml |
0.199 ml |
0.397 ml |
|
注意: |
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