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GR 159897

Catalog No. T15415Cas No. 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.

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Pack Size	Price	Availability	Quantity
1 mg	$110	35 days
5 mg	$458	35 days

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Product Introduction

Bioactivity

Description	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 bronch
In vitro	GR 159897 (10-30 μM; 72 hours; 4TBM, 4TLM, 4THM, and 4T1 cells) treatment enhances phosphorylation of P38. At the same time, it also 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 (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].
In vivo	GR 159897 (0.12 mg/kg; i.v.; guinea-pigs) treatment effectively antagonizes bronchoconstriction caused by GR64349. It has a long duration of action (3 h) [1].

Chemical Properties

Molecular Weight	414.54
Formula	C23H27FN2O2S
Cas No.	158848-32-9

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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