Catalog Number: 2602
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
  • M.Wt:
    584.67
  • Formula:
    C32H36N6O5
  • Solubility:
    Soluble to 100 mM in DMSO
  • Purity:
    >98%
  • Storage:
    Store at +4°C
  • CAS No:
    204067-01-6
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.
Background References
  1. PD 176252 - the first high affinity non-peptide gastrin-releasing peptide (BB2) receptor antagonist
    Ashwood et al.
    Bioorg.Med.Chem.Lett., 1998;8:2589
  2. Nonpeptide neuromedin B receptor antagonists inhibit the proliferation of C6 cells
    Moody et al.
    Eur.J.Pharmacol., 2000;409:133
  3. Nonpeptide gastrin releasing peptide receptor antagonists inhibit the proliferation of lung cancer cells
    Moody et al.
    Eur.J.Pharmacol., 2003;474:21
  4. Gastrin-releasing peptide/neuromedin B receptor antagonists pD176252, PD168368, and related analogs are potent agonists of human formyl-peptide receptors.
    Schepetkin et al.
    Mol.Pharmacol., 2011;79:77
Citations:

The citations listed below are publications that use Tocris products. Selected citations for PD 176252 include:

2 Citations: Showing 1 - 2
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  1. Circadian integration of glutamatergic signals by little SAAS in novel suprachiasmatic circuits.
    Authors: Atkins Et al.
    PLoS One 2010;5:e12612
  2. Characterization of putative GRP- and NMB-receptor antagonist's interaction with human receptors.
    Authors: González Et al.
    Peptides 2009;30:1473

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