PD 168368

• Product Name Alternative:

  OX2R antagonist

• UNSPSC Description:

  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].

• Target Antigen:

  Bombesin Receptor

• Type:

  Reference compound

• Related Pathways:

  GPCR/G Protein

• Field of Research:

  Cancer

• Assay Protocol:

  https://www.medchemexpress.com/pd-168368.html

• Purity:

  99.0

• Solubility:

  DMF : 10 mg/mL (ultrasonic;warming)|DMSO : 30 mg/mL (ultrasonic;warming)

• 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 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.

• Shipping Conditions:

  Blue Ice

• Storage Conditions:

  -20°C, 3 years (Powder)

• Clinical Information:

  No Development Reported

• CAS Number:

  204066-82-0