Biological Activity
A potent, selective, non-peptide, orally active neurokinin NK2 receptor antagonist. Competes for binding of [3H]GR100679 to hNK2-transfected CHO cells with a pKi of 9.5. Inhibits NK2 receptor-mediated contraction of guinea pig trachea with a pA2 of 8.7. Anxiolytic in vivo.
Licensing Information
Sold with the permission of GlaxoSmithKline
Compound Libraries
GR 159897 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 414.54 |
| Formula | C23H27FN2O2S |
| Storage | Desiccate at -20°C |
| Purity | ≥97% (HPLC) |
| CAS Number | 158848-32-9 |
| PubChem ID | 9953599 |
| InChI Key | BANYJBHWTOJQDU-GDLZYMKVSA-N |
| Smiles | FC1=CC=C2C(C(CCN3CCC(C[S@@+]([O-])C4=CC=CC=C4)(OC)CC3)=CN2)=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 20.73 | 50 | |
| ethanol | 4.15 | 10 |
Preparing Stock Solutions
The following data is based on the product molecular weight 414.54. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.41 mL | 12.06 mL | 24.12 mL |
| 5 mM | 0.48 mL | 2.41 mL | 4.82 mL |
| 10 mM | 0.24 mL | 1.21 mL | 2.41 mL |
| 50 mM | 0.05 mL | 0.24 mL | 0.48 mL |
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References
References are publications that support the products' biological activity.
Beresford et al (1995) GR 159897, a potent non-peptide antagonist at tachykinin NK2 receptors. Eur.J.Pharmacol. 272 241 PMID: 7713168
Walsh et al (1995) The anxiolytic-like activity of GR 159897, a non-peptide NK2 receptor antagonist, in rodent and primate models of anxiety. Psychopharmacology 121 186 PMID: 8545524
Cooper et al (1994) GR 159897 and related analogues as highly potent, orally active non-peptide neurokinin NK2 receptor antagonists. Bioorg.Med.Chem.Lett. 4 1951 PMID:
Keywords: GR 159897, supplier, Non-peptide, potents, NK2, antagonist, Tachykinin, Receptors, Neurokinin, GR159897, GlaxoSmithKline, GSK, NK2, Receptor, NK2, Receptor, Tocris Bioscience
