Biological Activity
Potent and selective NK3 receptor antagonist (Ki values are 0.26 and 19.3 nM in CHO cells expressing the human NK3 and NK2 receptor respectively). Also inhibits senktide-induced inositol monophosphate formation and intracellular calcium mobilization (IC50 = 10 nM).
Technical Data
| M. Wt | 658.11 |
| Formula | C35H42Cl2N4O2.HCl |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 264618-38-4 |
| PubChem ID | 90488827 |
| InChI Key | HYPKKQPFHSNZBY-GXUZKUJRSA-N |
| Smiles | O=C(N(C)C)NC1(C4=CC=CC=C4)CCN(CCC[C@]3(CN(C(C5=CC=CC=C5)=O)CCC3)[C@]2=CC=C(Cl)C(Cl)=C2)CC1.Cl |
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 | 65.81 | 100 | |
| ethanol | 65.81 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 658.11. 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 | 1.52 mL | 7.6 mL | 15.2 mL |
| 5 mM | 0.3 mL | 1.52 mL | 3.04 mL |
| 10 mM | 0.15 mL | 0.76 mL | 1.52 mL |
| 50 mM | 0.03 mL | 0.15 mL | 0.3 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Emonds-Alt et al (2002) Biochemical and pharmacological activities of SSR 146977, a new potent nonpeptide tachykinin NK3 receptor antagonist. Can.J.Physiol.Pharmacol. 80 482 PMID: 12056557
Keywords: SSR 146977 hydrochloride, supplier, tachykinin, neurokinin, receptors, nk3, neuropeptides, antagonists, SSR146977, NK3, Receptor, NK3, Receptor, Tocris Bioscience
