PD 168368

PD 168368 is a potent, competitive, and selective neuromedin B receptor (NMB-R) antagonist with the Ki of 15–45 nM[1]. PD 168368 is neuromedin B receptor (NMBR; IC50=96 nM) / gastrin-releasing peptide receptor (GRPR IC50=3500 nM) antagonist[2]. PD 168368 also is a mixed FPR1/FPR2/FPR3 agonist with EC50s of 0.57, 0.24, and 2.7 nM, respectively[3].

Product Specifications

CAS Number

[204066-82-0]

Product Name Alternative

OX2R antagonist

UNSPSC

12352005

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/pd-168368.html

Purity

99.0

Solubility

DMSO : 125 mg/mL (ultrasonic)

Smiles

O=C([C@](C)(CC1=CNC2=C1C=CC=C2)NC(NC3=CC=C(C=C3)[N+]([O-])=O)=O)NCC4(CCCCC4)C5=NC=CC=C5

Molecular Formula

C31H34N6O4

Molecular Weight

554.64

References & Citations

[1]R R Ryan, et al. Comparative pharmacology of the nonpeptide neuromedin B receptor antagonist PD 168368. J Pharmacol Exp Ther. 1999 Sep;290 (3) :1202-11.|[2]K Tokita, et al. Tyrosine 220 in the 5th transmembrane domain of the neuromedin B receptor is critical for the high selectivity of the peptoid antagonist PD168368. J Biol Chem. 2001 Jan 5;276 (1) :495-504.|[3]Igor A Schepetkin, 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.|[4]Hyun-Joo Park, et al. Neuromedin B receptor antagonism inhibits migration, invasion, and epithelial-mesenchymal transition of breast cancer cells. Int J Oncol. 2016 Sep;49 (3) :934-42.