GR 159897

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

GR 159897 

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。

GR 159897

GR 159897 Chemical Structure

CAS No. : 158848-32-9

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生物活性

GR 159897 is a highly potent, selective, competitive, brain-penetrated non-peptide neurokinin 2 (NK2) receptor antagonist. GR 159897 has little or no affinity for NK1 and NK3 receptors. GR 159897 inhibits binding of [3H]GR100679 to human NK2 (hNK2)-CHO cells and rat colon membranes with pKis 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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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.
参考文献

  • [1]. Beresford IJ, et al. GR159897, a potent non-peptide antagonist at tachykinin NK2 receptors. Eur J Pharmacol. 1995 Jan 16;272(2-3):241-8.

    [2]. Nizam E, et al. Differential consequences of neurokinin receptor 1 and 2 antagonists in metastatic breast carcinoma cells; Effects independent of Substance P. Biomed Pharmacother. 2018 Dec;108:263-270.

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