GR 159897

Name: GR 159897
Brand: TargetMol
SKU: T15415
Rating: 4.5 (1 reviews)

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产品编号 T15415Cas号 158848-32-9

GR 159897 is a competitive, brain-penetrated non-peptide NK2 receptor antagonist with anti-tumor effects. GR 159897 inhibits binding of [3H]GR100679 to human NK2-CHO cells and rat colon membranes (pKis: 9.51 and 10, respectively). It can antagonize bronchoconstriction.

GR 159897

还可以

产品编号 T15415Cas号 158848-32-9

规格	价格	库存	数量
1 mg	待估	35日内发货
5 mg	待估	35日内发货

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生物活性

产品描述	GR 159897 is a competitive, brain-penetrated non-peptide NK2 receptor antagonist with anti-tumor effects. GR 159897 inhibits binding of [3H]GR100679 to human NK2-CHO cells and rat colon membranes (pKis: 9.51 and 10, respectively). It can antagonize bronchoconstriction.
靶点活性	NK2:10 （pki）（ Rat colon membrane), NK2 (human):9.51（pki） (CHO cell)
体外活性	GR 159897 (10-30 μM; 72 hours; 4TBM, 4TLM, 4THM, and 4T1 cells) treatment enhances P38 phosphorylation and inhibits AKT activation in all metastatic cell lines, while ERK phosphorylation decreases in 4TBM, 4TLM, and 4THM cells but not in 4T1 cells. GR 159897 (10-30 μM; 72 hours; 4T1, 4THM, 4TLM, and 67NR cells) also inhibits cell proliferation dose-dependently in all lines, with a more pronounced effect in 4T1, 4THM, and 4TLM cells compared to 67NR cells [2].
体内活性	GR 159897 (0.12 mg/kg; i.v.; guinea-pigs) effectively antagonizes GR64349-induced bronchoconstriction with a long duration of action of 3 hours [1].