PD 176252

Pricing Availability Delivery Time Qty
Cat.No. 2602 - PD 176252 | C32H36N6O5 | CAS No. 204067-01-6
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)
Literature

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

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

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

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 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 1.71 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

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

Product Datasheets

Certificate of Analysis / Product Datasheet
Select another batch:
Safety Datasheet

References

References are publications that support the products' biological activity.

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.

View Related Products by Target

View Related Products by Product Action

View all Bombesin Receptor Antagonists

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

2 Citations for PD 176252

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.

Commented out for usability testing

Reviews

TODO: Add Reviews

Literature in this Area

GPCR

GPCR Product Listing

A collection of over 450 products for G protein-coupled receptors, the listing includes research tools for the study of:

  • Rhodopsin-like Receptors
  • Secretin-like Receptors
  • Glutamate Receptors
  • Frizzled Receptors
  • GPCR Signaling
Peptide Hormone Receptors

Peptide Hormone Receptors Product Listing

A collection of over 200 products for peptide hormone receptors, the listing includes research tools for the study of:

  • Anterior Pituitary Regulation
  • Blood Pressure Regulation
  • Feeding and Appetite Regulation
  • Glucose Regulation
  • Peptide Hormone Processing
Peptides Involved in Appetite Modulation

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.

Pathways for PD 176252

Protocols

TODO: Add Protocols