SDZ NKT 343

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Cat.No. 2394 - SDZ NKT 343 | C33H33N5O5 | CAS No. 180046-99-5
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)
Datasheet
Citations
Literature

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

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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.

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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Product Datasheets

Safety Datasheet

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


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Keywords: selective human NK1 antagonists Tachykinin Receptors Neurokinin SDZNKT343 NK1 Receptor

Citations for SDZ NKT 343

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