Description: Highly selective, human NK1 antagonist
Chemical Name: 1-[[(2-Nitrophenyl)amino]carbonyl]-L-prolyl-N-methyl-3-(2-naphthalenyl)-N-(phenylmethyl)-L-alaninamide
Purity: ≥98% (HPLC)
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
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.
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
Certificate of Analysis / Product Datasheet
Safety Datasheet
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References
References are publications that support the products' biological activity.
Walpoleet al (1998) Comparative, general pharmacology of SDZ NKT 343, a novel, selective NK1 receptor antagonist. Br.J.Pharmacol. 124 83 PMID: 9630347
Walpoleet 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
Campbellet 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