PD 176252

Cat. No. 2602

PD 176252 C32H36N6O5 [204067-01-6]

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Chemical Name: (S)-N-[[1-(5-Methoxy-2-pyridinyl)cyclohexyl]methyl]-α-methyl-α-[[[-(4-nitrophenyl)amino]carbonyl]amino-1H-indole-3-propanamide

Biological Activity

Non-peptide gastrin-releasing peptide receptor (GRP-R, BB2) and neuromedin B receptor (NMB-R, BB1) antagonist (Ki values are 0.17 and 1.0 nM for BB1 and BB2 respectively). Inhibits proliferation of rat C6 glioma cells (IC50 = 2 μM) and inhibits NCI-H1299 xenograft proliferation in nude mice (IC50 = 5 μM).

Technical Data

Soluble to 100 mM in DMSO
>98 %
Store at +4°C

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.

Certificate of Analysis / Product Datasheet / Safety Datasheet

Certificate of Analysis / Product Datasheet
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References are publications that support the products' biological activity.

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.

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

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

Ashwood et al (1998) PD 176252 - the first high affinity non-peptide gastrin-releasing peptide (BB2) receptor antagonist Bioorg.Med.Chem.Lett. 8 2589. PMID: 9873586.

If you know of a relevant reference for PD 176252 please let us know.

Citations are publications that use Tocris products. Selected citations for PD 176252 include:

Atkins et al (2010) Circadian integration of glutamatergic signals by little SAAS in novel suprachiasmatic circuits. PLoS One 5 e12612. PMID: 20830308.

González et al (2009) Characterization of putative GRP- and NMB-receptor antagonist's interaction with human receptors. Peptides 30 1473. PMID: 19463875.

Do you know of a great paper that uses PD 176252 from Tocris? If so please let us know.

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Keywords: PD 176252, supplier, GRP, BB2, NMB, BB1, receptor, antagonists, GRP-Preferring, Receptors, Gastrin-Releasing, Peptide-Preferring, NMB-Preferring, Neuromedin, B-Preferring, Bombesin, PD176252, Tocris Bioscience, Bombesin Receptor Antagonist products

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