PD 168368

Discontinued Product

PD 168368 (Cat. No. 2603) has been withdrawn from sale for commercial reasons.
Cat.No. 2603 - PD 168368 | C31H34N6O4 | CAS No. 204066-82-0
Description: Selective neuromedin B receptor antagonist (NMB-R, BB1)
Chemical Name: (S)-α-Methyl-α-[[[(4-nitrophenyl)amino]carbonyl]amino]-N-[[1-(2-pyridinyl)cyclohexyl]methyl]-1H-indole-3-propanamide
Purity: ≥96% (HPLC)
Datasheet
Citations
Reviews
Literature

Biological Activity

Potent neuromedin B receptor antagonist (NMB-R, BB1) (IC50 = 40 nM) that displays ~ 40-fold selectivity over the gastrin-releasing peptide receptor (GRP-R, BB2) and > 300-fold selectivity over BRS-R (bb3). Antagonizes neuromedin B-stimulated calcium release and inhibits proliferation of rat glioma cells (IC50 = 2 μM).

Technical Data

M. Wt 554.65
Formula C31H34N6O4
Storage Store at +4°C
Purity ≥96% (HPLC)
CAS Number 204066-82-0
Smiles O=C(NC3=CC=C([N+]([O-])=O)C=C3)N[C@@](C)(CC5=CNC4=CC=CC=C45)C(NCC1(C2=CC=CC=N2)CCCCC1)=O

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.

References

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

Ryan et al (1999) Comparative pharmacology of the nonpeptide neuromedin B receptor antagonist PD 168368 J.Pharmacol.Exp.Ther. 290 1202 PMID: 10454496

Moody et al (2000) Nonpeptide neuromedin B receptor antagonists inhibit the proliferation of C6 cells. Eur.J.Pharmacol. 409 133 PMID: 11104826

Moody et al (2003) Nonpeptide gastrin releasing peptide receptor antagonists inhibit the proliferation of lung cancer cells. Eur.J.Pharmacol. 474 21 PMID: 12909192

Schepetkin et al (2011) Gastrin-releasing peptide/neuromedin B receptor antagonists pD176252, PD168368, and related analogs are potent agonists of human formyl-peptide receptors. Mol.Pharmacol. 79 77 PMID: 20943772

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Keywords: PD 168368, PD 168368 supplier, Selective, neuromedin, B, receptor, antagonists, NMB-R, BB1, NMB-Preferring, Bombesin, PD168368, Receptors, 2603, Tocris Bioscience

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