GR 159897

• 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].

• UNSPSC :

  12352005

• Target :

  Neurokinin Receptor

• Type :

  Reference compound

• Related Pathways :

  GPCR/G Protein; Neuronal Signaling

• Applications :

  Metabolism-protein/nucleotide metabolism

• Field of Research :

  Cancer; Endocrinology; Neurological Disease

• Assay Protocol :

  https://www.medchemexpress.com/gr-159897.html

• Purity :

  99.60

• Solubility :

  DMSO : 31 mg/mL (ultrasonic; warming)

• Smiles :

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

• Molecular Formula :

  C23H27FN2O2S

• Molecular Weight :

  414.54

• References & Citations :

  [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.

• Shipping Conditions :

  Blue Ice

• Storage Conditions :

  -20°C (Powder, sealed storage, away from moisture)

• Scientific Category :

  Reference compound1

• Clinical Information :

  No Development Reported

• Isoform :

  NK2R

• CAS Number :

  [158848-32-9]