产品
编 号：F189083
分子式：C23H27FN2O2S
分子量：414.54
分子式：C23H27FN2O2S
分子量：414.54
产品类型
规格
价格
是否有货
10mg
询价
询价
结构图
CAS No: 158848-32-9
产品详情
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.
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).
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.
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.
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).
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.
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