158848-32-9
基本信息
5-Fluoro-3-[2-[4-methoxy-4-[[-phenylsulphinyl]methyl]-1-piperidinyl]ethyl]-1H-indole
(R)-5-Fluoro-3-[2-[4-methoxy-4-[(phenylsulfinyl)methyl]-1-piperidinyl]ethyl]-1H-indole
5-Fluoro-3-[2-[4-methoxy-4-[[(R)-phenylsulfinyl]methyl]-1-piperidinyl]ethyl]-1H-indole
5-FLUORO-3-[2-[4-METHOXY-4-[[(R)-PHENYLSULPHINYL]METHYL]-1-PIPERIDINYL]ETHYL]-1H-INDOLE
1H-Indole, 5-fluoro-3-[2-[4-methoxy-4-[[(R)-phenylsulfinyl]methyl]-1-piperidinyl]ethyl]-
物理化学性质
| 沸点 | 600.2±55.0 °C(Predicted) |
| 密度 | 1.29±0.1 g/cm3(Predicted) |
| 储存条件 | −20°C |
| 储存条件 | −20°C |
| 溶解度 | DMSO: ~24 mg/mL, soluble |
| 溶解度 | DMSO：~24 mg/mL |
| 酸度系数(pKa) | 16.46±0.30(Predicted) |
| 形态 | solid |
| 颜色 | off-white |
安全数据
| WGK Germany | 3 |
| WGK Germany | 3 |
常见问题列表
|
NK2 10 (pKi, Rat colon membrane) |
hNK2 9.51 (pKi, CHO cell) |
GR 159897 (10-30 μM; 72 hours; 4T1, 4THM, 4TLM and 67NR cells) treatment inhibits proliferation of cells in all cell lines dose- dependently, a response more pronounced in 4T1, 4THM and 4TLM cells compared to 67NR cells.
GR 159897 (10-30 μM; 72 hours; 4TBM, 4TLM, 4THM and 4T1 cells) treatment increases phosphorylation of P38, while inhibiting AKT activation in all metastatic cell lines whereas phosphorylation of ERK decreased in 4TBM, 4TLM and 4THM but not in 4T1 cells.
Cell Proliferation Assay
| Cell Line: | 4T1, 4THM, 4TLM and 67NR cells |
| Concentration: | 10 μM, 30 μM |
| Incubation Time: | 72 hours |
| Result: | Inhibited proliferation of cells in all cell lines dose- dependently, a response more pronounced in 4T1, 4THM and 4TLM cells compared to 67NR cells. |
Western Blot Analysis
| Cell Line: | 4TBM, 4TLM, 4THM and 4T1 cells |
| Concentration: | 10 μM, 30 μM |
| Incubation Time: | 40 hours |
| Result: | Increased phosphorylation of P38. |
GR 159897 (0.12 mg/kg; intravenous injection; guinea-pigs) treatment potently antagonizes bronchoconstriction induced by GR64349, with a long duration of action (3 h).
| Animal Model: | Guinea-pigs |
| Dosage: | 0.12 mg/kg |
| Administration: | Intravenous injection |
| Result: | Potently antagonised bronchoconstriction induced by GR64349, with a long duration of action (3 h). |