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PG 931 TFA

Names

[ CAS No. ]:
667430-81-1

[ Name ]:
PG 931 TFA

Biological Activity

[Description]:

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].

[Related Catalog]:

Research Areas >> Inflammation/Immunology
Signaling Pathways >> GPCR/G Protein >> Melanocortin Receptor

[Target]

IC50: 0.58 nM (melanocortin 4 receptor) IC50: 2.4 nM (melanocortin 5 receptor) IC50: 55 nM (melanocortin 3 receptor)[1]


[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: Wistar rats[2] Dosage: 13-108 nmol/kg Administration: Intravenous injection; single dose Result: Exhibitd an anti-shock effect occurred at nanomolar doses.

[References]

[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

Chemical & Physical Properties

[ Molecular Formula ]:
C59H85N15O11

[ Molecular Weight ]:
1180.40

[ Storage condition ]:
-20°C

Related Compounds