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| Product Name: | PG 931 | | Synonyms: | PG 931;L-Valinamide, N-acetyl-L-norleucyl-L-α-aspartyl-L-prolyl-D-phenylalanyl-L-arginyl-L-tryptophyl-L-lysyl-L-prolyl-, (2→7)-lactam;Ac-Nle-cyclo（Asp-Pro-D-Phe-Arg-Trp-Lys)-Pro-Val-NH2 | | CAS: | 667430-81-1 | | MF: | C59H85N15O11 | | MW: | 1180.42 | | EINECS: | | | Product Categories: | | | Mol File: | 667430-81-1.mol |  |
| | PG 931 Chemical Properties |
| 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 | | Sequence | Ac-{Nle}-Asp-Pro-{d-Phe}-Arg-Trp-Lys-Pro-Val-NH2 (Lactam bridge: Asp2-Lys7) |
| | PG 931 Usage And Synthesis |
| 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 |
| | PG 931 Preparation Products And Raw materials |
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