({1-[2-(5-氟-1H-吲哚-3-基)乙基]-4-甲氧基-4-哌啶基}甲基)(苯基)锍醇
中文名称 | ({1-[2-(5-氟-1H-吲哚-3-基)乙基]-4-甲氧基-4-哌啶基}甲基)(苯基)锍醇 |
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中文同义词 | ({1-[2-(5-氟-1H-吲哚-3-基)乙基]-4-甲氧基-4-哌啶基}甲基)(苯基)锍醇 |
英文名称 | 5-FLUORO-3-[2-[4-METHOXY-4-[[(R)-PHENYLSULPHINYL]METHYL]-1-PIPERIDINYL]ETHYL]-1H-INDOLE |
英文同义词 | 5-FLUORO-3-[2-[4-METHOXY-4-[[(R)-PHENYLSULPHINYL]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-[[-phenylsulphinyl]methyl]-1-piperidinyl]ethyl]-1H-indole;GR 159897;(R)-5-Fluoro-3-[2-[4-methoxy-4-[(phenylsulfinyl)methyl]-1-piperidinyl]ethyl]-1H-indole;1H-Indole, 5-fluoro-3-[2-[4-methoxy-4-[[(R)-phenylsulfinyl]methyl]-1-piperidinyl]ethyl]- |
CAS号 | 158848-32-9 |
分子式 | C23H27FN2O2S |
分子量 | 414.54 |
EINECS号 | |
相关类别 | |
Mol文件 | 158848-32-9.mol |
结构式 |
({1-[2-(5-氟-1H-吲哚-3-基)乙基]-4-甲氧基-4-哌啶基}甲基)(苯基)锍醇 性质
沸点 | 600.2±55.0 °C(Predicted) |
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密度 | 1.29±0.1 g/cm3(Predicted) |
储存条件 | −20°C |
溶解度 | DMSO:~24 mg/mL |
酸度系数(pKa) | 16.46±0.30(Predicted) |
形态 | 固体 |
颜色 | 米白色 |
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). |
安全信息
WGK Germany | 3 |
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提供商 | 语言 |
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英文
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