Chemical Properties | Back Directory | [density ]
1.41±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Soluble to 2 mg/ml in 25% ethanol / water | [form ]
Powder | [pka]
13.14±0.70(Predicted) | [color ]
White to off-white |
Hazard Information | Back Directory | [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) | [IC 50]
MC4R | [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 |
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