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GR 159897

Catalog No. T15415 CAS 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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GR 159897, CAS 158848-32-9

Pack Size	Availability	Price/USD	Quantity
1 mg	35 days	$ 110.00
5 mg	35 days	$ 458.00

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Storage & Solubility Information

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 bronchoconstriction.
Targets&IC50	NK2:10 （pki）（ Rat colon membrane), NK2 (human):9.51（pki） (CHO cell)
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].

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

Storage

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

References and Literature

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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Keywords

GR 159897 158848-32-9 Others GR159897 GR-159897 inhibitor inhibit

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