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PD 176252

Cat. No. 2602 2 Citations Submit a Review Datasheet / COA / SDS
Pricing Availability   Qty
Description: GRP (BB2) and NMB (BB1) receptor antagonist
Chemical Name: (S)-N-[[1-(5-Methoxy-2-pyridinyl)cyclohexyl]methyl]-α-methyl-α-[[[-(4-nitrophenyl)amino]carbonyl]amino-1H-indole-3-propanamide
Purity: ≥98% (HPLC)
Datasheet
Citations (2)
Reviews
Literature (1)
Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for PD 176252

PD 176252 is a 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 for PD 176252

M. Wt 584.67
Formula C32H36N6O5
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 204067-01-6
PubChem ID 9829828
InChI Key NNFUWNLENRUDHR-HKBQPEDESA-N
Smiles O=C(NC3=CC=C([N+]([O-])=O)C=C3)N[C@@](C)(CC5=CNC4=CC=CC=C45)C(NCC1(C2=CC=C(OC)C=N2)CCCCC1)=O

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 PD 176252

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 58.47 100

Preparing Stock Solutions for PD 176252

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.

Select a batch to recalculate based on the batch molecular weight:
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

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Product Datasheets for PD 176252

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References for PD 176252

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

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

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Peptides Involved in Appetite Modulation Scientific Review

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.