1. GPCR/G Protein
    Neuronal Signaling
  2. Neurokinin Receptor
  3. GR 159897

GR 159897 

Cat. No.: HY-107691
Handling Instructions

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.

For research use only. We do not sell to patients.

GR 159897 Chemical Structure

GR 159897 Chemical Structure

CAS No. : 158848-32-9

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Description

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)

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].

MCE 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.
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].

MCE 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).
Molecular Weight

414.54

Formula

C₂₃H₂₇FN₂O₂S

CAS No.

158848-32-9

SMILES

O=[[email protected]](CC1(OC)CCN(CCC2=CNC3=C2C=C(F)C=C3)CC1)C4=CC=CC=C4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

GR 159897GR159897GR-159897Neurokinin ReceptorNK receptorGR 64349non-peptidedurationbronchoconstrictiontachykininNK2anxiolytic-likeCNSP38anti-tumorInhibitorinhibitorinhibit

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GR 159897
Cat. No.:
HY-107691
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