网站主页 >> CAS数据库列表 >> ({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
({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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- CAS号:
- 158848-32-9
- 英文名:
- 5-FLUORO-3-[2-[4-METHOXY-4-[[(R)-PHENYLSULPHINYL]METHYL]-1-PIPERIDINYL]ETHYL]-1H-INDOLE
- 英文别名:
- GR 159897;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]-
- 中文名:
- ({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
- 中文别名:
- ({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
- CBNumber:
- CB3376531
- 分子式:
- C23H27FN2O2S
- 分子量:
- 414.54
- MOL File:
- 158848-32-9.mol
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({1-[2-(5-氟-1H-吲哚-3-基)乙基]-4-甲氧基-4-哌啶基}甲基)(苯基)锍醇化学性质
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沸点:
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600.2±55.0 °C(Predicted)
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密度:
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1.29±0.1 g/cm3(Predicted)
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储存条件:
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−20°C
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溶解度:
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DMSO: ~24 mg/mL, soluble
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酸度系数(pKa):
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16.46±0.30(Predicted)
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形态:
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solid
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颜色:
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off-white
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({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、用途与生产工艺
GR 159897 是一种高效，选择性，竞争性，可通过血脑屏障的非肽神经激肽 2 (NK2) 受体拮抗剂。GR 159897 对 NK1 和 NK3 受体几乎没有亲和力。GR 159897 抑制 [3H]GR100679 与人 NK2-CHO 细胞和大鼠结肠膜的结合，pKi 值分别为 9.51 和 10。拮抗支气管收缩。抗焦虑和抗肿瘤作用。
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NK2
10 (pKi, Rat colon membrane)
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hNK2
9.51 (pKi, CHO cell)
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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
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Cell Line:
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4T1, 4THM, 4TLM and 67NR cells
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Concentration:
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10 μM, 30 μM
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Incubation Time:
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72 hours
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Result:
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Inhibited proliferation of cells in all cell lines dose- dependently, a response more pronounced in 4T1, 4THM and 4TLM cells compared to 67NR cells.
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Western Blot Analysis
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Cell Line:
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4TBM, 4TLM, 4THM and 4T1 cells
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Concentration:
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10 μM, 30 μM
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Incubation Time:
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40 hours
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Result:
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Increased phosphorylation of P38.
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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).
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Animal Model:
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Guinea-pigs
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Dosage:
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0.12 mg/kg
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Administration:
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Intravenous injection
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Result:
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Potently antagonised bronchoconstriction induced by GR64349, with a long duration of action (3 h).
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({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
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
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| 2024/01/25 | HY-107691 | GR 159897 | | 10 mg | 6048元 |
({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
生产厂家
158848-32-9, ({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 相关搜索:
- C23H27FN2O2S
- C23H27O2N2SF
- ({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
- 158848-32-9
- 1H-Indole, 5-fluoro-3-[2-[4-methoxy-4-[[(R)-phenylsulfinyl]methyl]-1-piperidinyl]ethyl]-
- (R)-5-Fluoro-3-[2-[4-methoxy-4-[(phenylsulfinyl)methyl]-1-piperidinyl]ethyl]-1H-indole
- GR 159897
- 5-Fluoro-3-[2-[4-methoxy-4-[[-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-[[(R)-PHENYLSULPHINYL]METHYL]-1-PIPERIDINYL]ETHYL]-1H-INDOLE