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ChemicalBook--->CAS DataBase List--->667430-81-1

667430-81-1

667430-81-1 Structure

667430-81-1 Structure
IdentificationBack Directory
[Name]

PG 931
[CAS]

667430-81-1
[Synonyms]

PG 931
[Molecular Formula]

C59H85N15O11
[MOL File]

667430-81-1.mol
[Molecular Weight]

1180.42
Chemical PropertiesBack 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 InformationBack 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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