Biological Activity
Highly selective human tachykinin NK1 receptor antagonist (IC50 values are 0.62 and 451 nM for human and rat receptors respectively) that displays > 130-fold selectivity over human NK2 and NK3 receptors. Potently antagonizes SP-induced Ca2+ efflux in vitro and inhibits mechanical hyperalgesia in vivo.
Compound Libraries
SDZ NKT 343 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 579.65 |
| Formula | C33H33N5O5 |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 180046-99-5 |
| PubChem ID | 9851211 |
| InChI Key | PCVSIMQAFWRUEC-JDXGNMNLSA-N |
| Smiles | O=C(NC3=C([N+]([O-])=O)C=CC=C3)N1[C@H]([C@@](N[C@H]([C@@](N(C)CC4=CC=CC=C4)=O)CC2=CC=C(C=CC=C5)C5=C2)=O)CCC1 |
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 | 57.97 | 100 | |
| ethanol | 57.97 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 579.65. 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 | 1.73 mL | 8.63 mL | 17.25 mL |
| 5 mM | 0.35 mL | 1.73 mL | 3.45 mL |
| 10 mM | 0.17 mL | 0.86 mL | 1.73 mL |
| 50 mM | 0.03 mL | 0.17 mL | 0.35 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Walpole et al (1998) Comparative, general pharmacology of SDZ NKT 343, a novel, selective NK1 receptor antagonist. Br.J.Pharmacol. 124 83 PMID: 9630347
Walpole et al (1998) 2-Nitrophenylcarbamoyl-(S)-prolyl-(S)-3-(2-naphthyl)alanyl-N-benzyl-N-methylamide (SDZ NKT 343), a potent human NK1 tachykinin receptor antagonist with good oral analgesic activity in chronic pain models. J.Med.Chem. 41 3159 PMID: 9703462
Campbell et al (1998) Selective neurokinin-1 receptor antagonists are anti-hyperalgesic in a model of neuropathic pain in the guinea-pig. Neuroscience. 87 527 PMID: 9758219
Keywords: SDZ NKT 343, supplier, selective, human, NK1, antagonists, Tachykinin, Receptors, Neurokinin, SDZNKT343, NK1, Receptor, NK1, Receptor, Tocris Bioscience
