204066-82-0
Chemical Structure
PD 168368
- CAS No.: 204066-82-0
- Formula:C31H34N6O4
- Molecular Weight:554.64
IUPAC Name: (S)-3-(1H-indol-3-yl)-2-methyl-2-(3-(4-nitrophenyl)ureido)-N-((1-(pyridin-2-yl)cyclohexyl)methyl)propanamide
InChIKey: AFDXUTWMFMAQJO-PMERELPUSA-N
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
Biological Activity: 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].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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PD 168368 | 98.11% | PD 168368 is a potent, competitive, and selective neuromedin B receptor (NMB-R) antagonist with the Ki of 15–45 nM. PD 168368 is neuromedin B receptor (NMBR; IC50=96 nM) / gastrin-releasing peptide receptor (GRPR IC50=3500 nM) antagonist. PD 168368 also is a mixed FPR1/FPR2/FPR3 agonist with EC50s of 0.57, 0.24, and 2.7 nM, respectively. | ||||||||||||||||||||
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References
- [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. [Content Brief]
- [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. [Content Brief]
- [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. [Content Brief]
