Etalocib
| 中文名称 | Etalocib |
|---|---|
| 中文同义词 | 2-(3-(3-((5-乙基-4'-氟-2-羟基-[1,1'-联苯]-4-基)氧基)丙氧基)-2-丙基苯氧基)苯甲酸;化合物ETALOCIB;LY293111,白三烯 (LTB4) 受体的拮抗剂;2-[2-丙基-3-[3-[2-乙基-4-(4-氟苯基)-5-羟基苯氧基]丙氧基]苯氧基]苯甲酸;2-(3-(3-((5-乙基-4'-氟-2-羟基-[1,1'-联苯]-4-基)氧基)丙氧基)-2-丙基苯氧基)苯甲酸 |
| 英文名称 | Etalocib |
| 英文同义词 | Etalocib;LY293111;VML 295;2-(3-(3-((5-Ethyl-4'-fluoro-2-hydroxy-[1,1'-biphenyl]-4-yl)oxy)propoxy)-2-propylphenoxy)benzoic acid;Benzoic acid, 2-[3-[3-[(5-ethyl-4'-fluoro-2-hydroxy[1,1'-biphenyl]-4-yl)oxy]propoxy]-2-propylphenoxy]-;LY293111 Exclusive;YFIZRWPXUYFCSN-UHFFFAOYSA-N;Etalocib(LY293111) |
| CAS号 | 161172-51-6 |
| 分子式 | C33H33FO6 |
| 分子量 | 544.61 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 161172-51-6.mol |
| 结构式 |  |
Etalocib 性质
| 熔点 | 68-70 °C(Solv: acetonitrile (75-05-8)) |
|---|---|
| 沸点 | 656.8±55.0 °C(Predicted) |
| 密度 | 1?+-.0.06 g/cm3(Predicted) |
| 储存条件 | Store at -20°C |
| 溶解度 | DMSO：98.5（最大浓度 mg/mL）；173.85（最大浓度 mM） |
| 酸度系数(pKa) | 3.32±0.36(Predicted) |
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. |
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/01/25 | HY-13628 | Etalocib | 1 mg | 1680元 | |
| 2024/01/25 | HY-13628 | Etalocib Etalocib | 161172-51-6 | 5mg | 4200元 |