Biological Activity
Potent, selective and competitive non-peptide NK3 receptor antagonist (Ki = 13 nM at hNK3). Displays 90-fold and 7000-fold selectivity over hNK2 and hNK1 receptors respectively. Active in vivo, inhibiting agonist-induced pupillary constriction.
Licensing Information
Sold under license
Compound Libraries
SB 218795 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 396.44 |
| Formula | C25H20N2O3 |
| Storage | Store at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 174635-53-1 |
| PubChem ID | 6604858 |
| InChI Key | IUMQXQJZIHWLIN-HSZRJFAPSA-N |
| Smiles | COC(=O)[C@H](NC(=O)C1=C2C=CC=CC2=NC(=C1)C1=CC=CC=C1)C1=CC=CC=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
| Solubility | Soluble to 100 mM in DMSO and to 5 mM in ethanol |
Preparing Stock Solutions
The following data is based on the product molecular weight 396.44. 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 | 2.52 mL | 12.61 mL | 25.22 mL |
| 5 mM | 0.5 mL | 2.52 mL | 5.04 mL |
| 10 mM | 0.25 mL | 1.26 mL | 2.52 mL |
| 50 mM | 0.05 mL | 0.25 mL | 0.5 mL |
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References
References are publications that support the products' biological activity.
Giardina et al (1997) Discovery of a novel class of selective non-peptide antagonists for the human neurokinin-3 receptor. 1. Identification of the 4-quinolinecarboxamide framework. J.Med.Chem. 40 1794 PMID: 9191956
Medhurst et al (1997) In vitro and in vivo characterization of NK3 receptors in the rabbit eye by use of selective non-peptide NK3 receptor antagonists. Br.J.Pharmacol. 122 469 PMID: 9351503
Keywords: SB 218795, supplier, Potent, selective, non-peptide, NK3, antagonists, Tachykinin, Receptors, Neurokinin, SB218795, NK3, Receptor, NK3, Receptor, Tocris Bioscience
