PD176252

PD176252 is a potent antagonist of neuromedin-B preferring (BB1) and gastrin-releasing peptide-preferring (BB2) receptor with Kis of 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; PD176252 is also an agonist of N-Formyl peptide receptor1/2 (FPR1/FPR2), with EC50s of 0.31 and 0.66 μM in HL-60 cells.

Product Specifications

CAS Number

[204067-01-6]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Bombesin Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/PD176252.html

Purity

99.38

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C(NC1=CC=C([N+]([O-])=O)C=C1)N[C@](CC2=CNC3=C2C=CC=C3)(C)C(NCC4(C5=CC=C(OC)C=N5)CCCCC4)=O

Molecular Formula

C32H36N6O5

Molecular Weight

584.67

Precautions

H302, H315, H319, H335

References & Citations

[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.