TargetMol

PD176252

Product Code:
 
TAR-T16449
Product Group:
 
Inhibitors and Activators
Supplier:
 
TargetMol
Regulatory Status:
 
RUO
Shipping:
 
cool pack
Storage:
 
-20℃
1 / 1
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Further Information

Bioactivity:
PD176252 is also an agonist of N-Formyl peptide receptor1/2 (EC50s: 0.31 and 0.66 μM in HL-60 cells). PD176252 is an effective antagonist of neuromedin-B preferring (BB1) and gastrin-releasing peptide-preferring (BB2) receptor (Kis: 0.17 nM and 1 nM for human BB1 and BB2 receptors, and 0.66 nM, 16 nM for Rat BB1 and BB2 receptors, respectively).
CAS:
204067-01-6
Formula:
C32H36N6O5
Molecular Weight:
584.677
Purity:
0.98
SMILES:
COc1ccc(nc1)C1(CNC(=O)[C@](C)(Cc2c[nH]c3ccccc23)NC(=O)Nc2ccc(cc2)[N+]([O-])=O)CCCCC1

References

1. Ashwood V, et al. PD 176252--the first high affinity non-peptide gastrin-releasing peptide (BB2) receptor antagonist. Bioorg Med Chem Lett. 1998 Sep 22;8(18):2589-94. 2. Schepetkin IA, et al. Gastrin-releasing peptide/neuromedin B receptor antagonists PD176252, PD168368, and related analogs are potent agonists of human formyl-peptide receptors. Mol Pharmacol. 2011 Jan;79(1):77-90. 3. Moody TW, et al. Nonpeptide gastrin releasing peptide receptor antagonists inhibit the proliferation of lung cancer cells. Eur J Pharmacol. 2003 Aug 1;474(1):21-9.