Uses
PG-931, an analog of SHU 9119 (HY-P0227), is a potent melanocortin 4 (MC4) receptor (IC50=0.58 nM) agonist and is more selective than for the hMC3R (IC50=55 nM) or the hMC5R (IC50=2.4 nM). PG-931 can reverse haemorrhagic shock and prevent multiple organ damage in vivo[2].
Biological Activity
PG-931 is an analog of SHU 9119 (HY-P0227). PG-931 is a potent melanocortin 4 (MC4) receptor (IC50=0.58 nM) agonist, more selective than hMC3R (IC50=55 nM) or hMC5R (IC50=2.4 nM). It can reverse hemorrhagic shock and prevent multiple organ damage in vivo in animal experimental models.
in vivo
PG-931 (intravenous injection; 13-10 8 nmol/kg; single dose) produces a dose-dependent restoration of cardiovascular and respiratory functions, and improved survival in Wistar rats with haemorrhagic shock.
| Animal Model: | Wistar rats |
| Dosage: | 13-10 8 nmol/kg |
| Administration: | Intravenous injection; single dose |
| Result: | Exhibitd an anti-shock effect occurred at nanomolar doses. |
target
IC50: 0.58 nM (melanocortin 4 receptor)IC50: 2.4 nM (melanocortin 5 receptor)IC50: 55 nM (melanocortin 3 receptor)
References
[1] D Giuliani, et al. Selective melanocortin MC4 receptor agonists reverse haemorrhagic shock and prevent multiple organ damage. Br J Pharmacol DOI:
10.1038/sj.bjp.0707115[2] P Grieco, et al. Extensive structure-activity studies of lactam derivatives of MT-II and SHU-9119: their activity and selectivity at human melanocortin receptors 3, 4, and 5. J Pept Res DOI:
10.1034/j.1399-3011.2003.00087.x
