A peptide MC4R agonist
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PG-931

Item No. 41551

Technical Information
Formal Name
(2→7)-lactam N-acetyl-L-norleucyl-L-α-aspartyl-L-prolyl-D-phenylalanyl-L-arginyl-L-tryptophyl-L-lysyl-L-prolyl-L-valinamide
CAS Number
667430-81-1
Synonyms
  • Ac-Nle-cyclic[Asp-Pro-D-Phe-Arg-Trp-Lys]-Pro-Val-NH2
Molecular Formula
C59H85N15O11
Formula Weight
Purity
≥98%
A neat oil
Peptide Sequence
Ac-Nle-c[DPfRWK]-PV-NH2
DMSO: Soluble: ≥10 mg/ml
SMILES
O=C(N[C@@H](CCCCNC(C[C@@H](C(N1[C@](CCC1)([H])C(N[C@@H](C(N[C@H](C(N2)=O)CCCNC(N)=N)=O)CC3=CC=CC=C3)=O)=O)NC([C@@H](NC(C)=O)CCCC)=O)=O)C(N4[C@@H](CCC4)C(N[C@H](C(N)=O)C(C)C)=O)=O)[C@@H]2CC5=CNC6=CC=CC=C56
InChi Code
InChI=1S/C59H85N15O11/c1-5-6-20-40(66-35(4)75)51(78)71-45-32-48(76)63-26-13-12-22-42(57(84)73-28-16-25-47(73)56(83)72-49(34(2)3)50(60)77)68-54(81)44(31-37-33-65-39-21-11-10-19-38(37)39)69-52(79)41(23-14-27-64-59(61)62)67-53(80)43(30-36-17-8-7-9-18-36)70-55(82)46-24-15-29-74(46)58(45)85/h7-11,17-19,21,33-34,40-47,49,65H,5-6,12-16,20,22-32H2,1-4H3,(H2,60,77)(H,63,76)(H,66,75)(H,67,80)(H,68,81)(H,69,79)(H,70,82)(H,71,78)(H,72,83)(H4,61,62,64)/t40-,41-,42-,43+,44-,45-,46-,47-,49-/m0/s1
InChi Key
WOFDJLFPEWSAPJ-YEJBJNCVSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    Product Description

    PG-931 is a peptide agonist of melanocortin receptor 4 (MC4R).1 It increases intracellular cAMP levels in CHO cells expressing MC4R with an EC50 value of 0.42 nM. PG-931 selectively binds to MC4R over MC3R and MC5R (IC50s = 0.58, 55, and 2.4 nM, respectively). It increases mean arterial pressure (MAP), pulse pressure, and respiratory rate in a rat model of hemorrhagic shock in a dose-dependent manner.2 It also prevents multiple organ damage and increases survival in the same model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Grieco, P., Balse-Srinivasan, P., Han, G., et alExtensive 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. 62(5), 199-206 (2003).

    2. Giuliani, D., Mioni, C., Bazzani, C., et alSelective melanocortin MC4 receptor agonists reverse haemorrhagic shock and prevent multiple organ damage. Br. J. Pharmacol. 150(5), 595-603 (2007).