PG-901 is a full, selective MC5R agonist ( EC 50 = 0.072 nM for hMC5R). PG-901 is also a full antagonist at the hMC3R and the hMC4R ( K b: 1.0 nM and 0.53 nM, respectively). PG-901 significantly diminishes Cytokines ( IL-1α, IL-1β, IL-6 ). PG-901 increases glucose tolerance, reduces blood glucose, decreases retinal damage [1] [2] [3].
References:
[1]. Grieco P, et al. Design and synthesis of highly potent and selective melanotropin analogues of SHU9119 modified at position 6. Biochem Biophys Res Commun. 2002 Apr 12;292(4):1075-80.
[2]. Swan P, et al. α-Melanocyte Stimulating Hormone Reduces Blood Glucose Across Species. bioRxiv, 2025: 2025.03. 26.645414.
[3]. Rossi S, et al. Activation of Melanocortin Receptors MC 1 and MC 5 Attenuates Retinal Damage in Experimental Diabetic Retinopathy. Mediators Inflamm. 2016;2016:7368389.
References:
[1]. Grieco P, et al. Design and synthesis of highly potent and selective melanotropin analogues of SHU9119 modified at position 6. Biochem Biophys Res Commun. 2002 Apr 12;292(4):1075-80.
[2]. Swan P, et al. α-Melanocyte Stimulating Hormone Reduces Blood Glucose Across Species. bioRxiv, 2025: 2025.03. 26.645414.
[3]. Rossi S, et al. Activation of Melanocortin Receptors MC 1 and MC 5 Attenuates Retinal Damage in Experimental Diabetic Retinopathy. Mediators Inflamm. 2016;2016:7368389.