| Bioactivity | 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]. | ||||||
| Target | IC50: 0.58 nM (melanocortin 4 receptor)IC50: 2.4 nM (melanocortin 5 receptor)IC50: 55 nM (melanocortin 3 receptor) | ||||||
| In Vivo | PG-931 (intravenous injection; 13-108 nmol/kg; single dose) produces a dose-dependent restoration of cardiovascular and respiratory functions, and improved survival in Wistar rats with haemorrhagic shock[2]. Animal Model: | ||||||
| Name | PG-931 | ||||||
| CAS | 667430-81-1 | ||||||
| Shortening | Ac-{Nle}-DP-{D-Phe}-RWKPV-NH2 (Lactam bridge:Asp2-Lys7) | ||||||
| Formula | C59H85N15O11 | ||||||
| Molar Mass | 1180.40 | ||||||
| Appearance | Solid | ||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||
| Storage | Sealed storage, away from moisture and light, under nitrogen
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen) |
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| Reference | [1]. D Giuliani, et al. Selective melanocortin MC4 receptor agonists reverse haemorrhagic shock and prevent multiple organ damage. Br J Pharmacol [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 |