161172-51-6
161172-51-6 結構式
基本信息
2-(3-(3-((5-乙基-4'-氟-2-羥基-[1,1'-聯(lián)苯]-4-基)氧基)丙氧基)-2-丙基苯氧基)苯甲酸
LY293111
Etalocib
LY293111 Exclusive
YFIZRWPXUYFCSN-UHFFFAOYSA-N
Benzoic acid, 2-[3-[3-[(5-ethyl-4'-fluoro-2-hydroxy[1,1'-biphenyl]-4-yl)oxy]propoxy]-2-propylphenoxy]-
物理化學性質
常見問題列表
Etalocib (LY293111) elicits a concentration-dependent inhibition of LTB
4
induced CD11b up-regulation.
Etalocib (LY293111) is an extremely potent and selective antagonist of human neutrophil function in vitro.
Etalocib (LY293111, 250 and 500 nM, 24-72 h) induces apoptosis and inhibits proliferation in human pancreatic cancer cells.
Cell Proliferation Assay
| Cell Line: | MiaPaCa-2 and AsPC-1 human pancreatic cancer cells. [3] |
| Concentration: | 500 nM. |
| Incubation Time: | 24, 48, and 72 h. |
| Result: | Caused both a concentration-dependent and time-dependent inhibition of thymidine incorporation in both MiaPaCa-2 and AsPC-1 human pancreatic cancer cells. |
Apoptosis Analysis
| Cell Line: | MiaPaCa-2 and AsPC-1 human pancreatic cancer cells. |
| Concentration: | 250 and 500 nM. |
| Incubation Time: | 24 h. |
| Result: | Induced apoptosis in human pancreatic cancer cells. |
Etalocib (LY293111) produces a dose-related inhibition of acute leukotriene B
4
-induced airway obstruction when administered i.v. (ED
50
=14 μg/kg) or p.o. (ED
50
=0.4 mg/kg).
Etalocib (LY293111, 10 mg/kg) inhibits A23187-induced lung inflammatory changes at 1 h.
Etalocib (LY293111, 250 mg/kg/day, orally) inhibits growth of human pancreatic cancer xenografts in athymic mice.
| Animal Model: |
Guinea pigs.
|
| Dosage: | 1-10 mg/kg. |
| Administration: | Orally once. |
| Result: |
A single 1 mg/kg oral dose inhibited excised lung gas volume increases by 76.7±7.1% (n=4, P<0.002) when given 8 h prior to leukotriene B
4
challenge, and 28.6±20.3% (n=4, NS) when given 24 h before challenge.
Had no effect (10 mg/kg) on pulmonary gas trapping at 1 h or 2 h after A23187 challenge. However, at 4 h, the pulmonary gas trapping response was significantly less than that of vehicle-treated controls and not different from sham values. The 10 mg/kg dose inhibited A23187-induced lung inflammatory changes at 1 h, but was without effect at 2 h or 4 h after challenge. |