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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).
|Storage||Store at +4°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 584.67. 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.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.71 mL||8.55 mL||17.1 mL|
|5 mM||0.34 mL||1.71 mL||3.42 mL|
|10 mM||0.17 mL||0.86 mL||1.71 mL|
|50 mM||0.03 mL||0.17 mL||0.34 mL|
References are publications that support the biological activity of the product.
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
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
If you know of a relevant reference for PD 176252, please let us know.
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Keywords: PD 176252, PD 176252 supplier, GRP, BB2, NMB, BB1, receptor, antagonists, GRP-Preferring, Receptors, Gastrin-Releasing, Peptide-Preferring, NMB-Preferring, Neuromedin, B-Preferring, Bombesin, PD176252, 2602, Tocris Bioscience
2 Citations for PD 176252
Citations are publications that use Tocris products. Selected citations for PD 176252 include:
González et al (2009) Characterization of putative GRP- and NMB-receptor antagonist's interaction with human receptors. Peptides 30 1473 PMID: 19463875
Atkins et al (2010) Circadian integration of glutamatergic signals by little SAAS in novel suprachiasmatic circuits. PLoS One 5 e12612 PMID: 20830308
Do you know of a great paper that uses PD 176252 from Tocris? Please let us know.
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Literature in this Area
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Peptides Involved in Appetite Modulation Scientific Review
Written by Sonia Tucci, Lynsay Kobelis and Tim Kirkham, this review provides a synopsis of the increasing number of peptides that have been implicated in appetite regulation and energy homeostasis; putative roles of the major peptides are outlined and compounds available from Tocris are listed.