({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號(hào):
- 158848-32-9
- 英文名:
- 5-FLUORO-3-[2-[4-METHOXY-4-[[(R)-PHENYLSULPHINYL]METHYL]-1-PIPERIDINYL]ETHYL]-1H-INDOLE
- 英文別名:
- 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
- 中文別名:
- ({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)锍醇化學(xué)性質(zhì)
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沸點(diǎn):
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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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儲(chǔ)存條件:
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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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酸度系數(shù)(pKa):
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16.46±0.30(Predicted)
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形態(tài):
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solid
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顏色:
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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)锍醇性質(zhì)、用途與生產(chǎn)工藝
GR 159897 是一種高效，選擇性，競(jìng)爭(zhēng)性，可通過(guò)血腦屏障的非肽神經(jīng)激肽 2 (NK2) 受體拮抗劑。GR 159897 對(duì) NK1 和 NK3 受體幾乎沒(méi)有親和力。GR 159897 抑制 [3H]GR100679 與人 NK2-CHO 細(xì)胞和大鼠結(jié)腸膜的結(jié)合，pKi 值分別為 9.51 和 10。拮抗支氣管收縮?？菇箲]和抗腫瘤作用。
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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
上下游產(chǎn)品信息
上游原料
下游產(chǎn)品
| 更新日期 | 產(chǎn)品編號(hào) | 產(chǎn)品名稱 | CAS編號(hào) | 包裝 | 價(jià)格 |
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| 2025/05/22 | HY-107691 | ({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
GR 159897 | 158848-32-9 | 1 mg | 1200元 |
| 2025/05/22 | HY-107691 | ({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
GR 159897 | 158848-32-9 | 5 mg | 3080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
生產(chǎn)廠家
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 相關(guān)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