({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

生物活性靶点体外研究体内研究 ({1-[2-(5-氟-1H-吲哚-3-基)乙基]-4-甲氧基-4-哌啶基}甲基)(苯基)锍醇试剂级价格

CAS号:158848-32-9
英文名:5-FLUORO-3-[2-[4-METHOXY-4-[[(R)-PHENYLSULPHINYL]METHYL]-1-PIPERIDINYL]ETHYL]-1H-INDOLE
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
CBNumber:CB3376531
分子式:C23H27FN2O2S
分子量:414.54
MOL File:158848-32-9.mol

({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

沸点 :600.2±55.0 °C(Predicted)
密度 :1.29±0.1 g/cm3(Predicted)
储存条件 :−20°C
溶解度 :DMSO: ~24 mg/mL, soluble
酸度系数(pKa) :16.46±0.30(Predicted)
形态 :solid
颜色 :off-white

安全信息

WGK Germany :3

({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

生物活性 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。
靶点

NK2

10 (pKi, Rat colon membrane)

hNK2

9.51 (pKi, CHO cell)

体外研究

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.

体内研究

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).