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GR 159897
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
GR 159897图片
CAS NO:158848-32-9
包装与价格：
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
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。
生物活性

GR 159897 is a highly potent, selective, competitive, brain-penetrated non-peptideneurokinin 2 (NK2) receptorantagonist. GR 159897 has little or no affinity for NK1and NK3receptors. GR 159897 inhibits binding of [3H]GR100679 tohuman NK2(hNK2)-CHO cells and rat colon membranes withpKis of 9.51 and 10, respectively. Antagonizes bronchoconstriction. Anxiolytic-like and anti-tumor effects[1][2].

IC50& Target[1]

NK2

10 (pKi, Rat colon membrane)

hNK2

9.51 (pKi, CHO cell)

体外研究
(In Vitro)

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[2].
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[2].

Cell Proliferation Assay[2]

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[2]

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
(In Vivo)

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)[1].

Animal Model:Guinea-pigs[1]
Dosage:0.12 mg/kg
Administration:Intravenous injection
Result:Potently antagonised bronchoconstriction induced by GR64349, with a long duration of action (3 h).
分子量

414.54

Formula

C23H27FN2O2S

CAS 号

158848-32-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.