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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)
Literature (2)

Biological Activity for SDZ NKT 343

SDZ NKT 343 is a 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 for SDZ NKT 343

SDZ NKT 343 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for SDZ NKT 343

M. Wt 579.65
Formula C33H33N5O5
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 180046-99-5
PubChem ID 9851211
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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for SDZ NKT 343

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 57.97 100
ethanol 57.97 100

Preparing Stock Solutions for SDZ NKT 343

The following data is based on the product molecular weight 579.65. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
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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References for SDZ NKT 343

References are publications that support the biological activity of the product.

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

If you know of a relevant reference for SDZ NKT 343, please let us know.

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Keywords: SDZ NKT 343, SDZ NKT 343 supplier, selective, human, NK1, antagonists, Tachykinin, Receptors, Neurokinin, SDZNKT343, Receptor, 2394, Tocris Bioscience

Citations for SDZ NKT 343

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