α-msh tfa

α-Melanocyte-stimulating hormone (α-MSH) is a 13-amino acid peptide hormone produced by post-translational processing of proopiomelanocortin (POMC) in the pituitary gland, as well as in keratinocytes, astrocytes, monocytes, and gastrointestinal cells.1It is an agonist of melanocortin receptor 3 (MC3R) and MC4R that induces cAMP production in Hepa cells expressing the human receptors (EC50s = 0.16 and 56 nM, respectively).2α-MSH (100 pM) reducesS. aureuscolony formation andC. albicansgerm tube formationin vitro.3It inhibits endotoxin-, ceramide-, TNF-α-, or okadaic acid-induced activation of NF-κB in U937 cells.1α-MSH reduces IL-6- or TNF-α-induced ear edema in mice.4It also prevents the development of adjuvant-induced arthritis in rats and increases survival in a mouse model of septic shock. Increased plasma levels of α-MSH are positively correlated with delayed disease progression and reduced death in patients with HIV.1 1.Catania, A., Airaghi, L., Colombo, G., et al.α-melanocyte-stimulating hormone in normal human physiology and disease statesTrends Endocrinol. Metab.11(8)304-308(2000) 2.Miwa, H., Gantz, I., Konda, Y., et al.Structural determinants of the melanocortin peptides required for activation of melanocortin-3 and melanocortin-4 receptorsJ. Pharmacol. Exp. Ther.273(1)367-372(1995) 3.Cutuli, M., Cristiani, S., Lipton, J.M., et al.Antimicrobial effects of a-MSH peptidesJ. Leukoc. Biol.67(2)233-239(2000) 4.Lipton, J.M., Ceriani, G., Macaluso, A., et al.Antiiinflammatory effect of the neuropeptide a-MSH in acute, chronic, and systemic inflammationAnn. N.Y. Acad. Sci.25(741)137-148(1994)

β-Melanocyte Stimulating Hormone (MSH), human TFA, is a 22-residue peptide that functions as an endogenous agonist for the melanocortin-4 receptor (MC4-R) [1].

Lys-γ3-MSH(human) TFA, a melanocortin peptide originating from the C-terminal fragment of pro-opiomelanocortin (POMC), enhances the steroidogenic response of rat adrenal glands to adrenocorticotrophin (ACTH). It is a potent stimulator of lipolysis, demonstrating an apparent EC50 of 3.56 nM, by activating hormone-sensitive lipase (HSL) and Perilipin A, leading to lipolysis [1] [2].

[D-Trp8]-γ-MSH TFA is a potent, selective agonist for the melanocortin 3 (MC3) receptor, demonstrating IC50 values of 6.7 nM for hMC3, 600 nM for hMC4, and 340 nM for hMC5 in CHO cells, respectively. It shows potential in providing protection against various inflammatory disorders, including rheumatoid arthritis and colitis [1] [2].

γ1-MSH TFA, a melanocortin MC3 receptor agonist, demonstrates a binding affinity (K i) of 34 nM for the rat MC3 receptor. Notably, it exhibits approximately 40-fold greater selectivity for the MC3 receptor compared to the MC4 receptor, with a K i of 1318 nM for MC4 [1].

β-Melanocyte Stimulating Hormone (MSH), human (Synonyms: Beta-MSH (1-22) (human)) β-Melanocyte Stimulating Hormone (MSH), human, a 22-residue peptide, acts as an endogenous melanocortin-4 receptor (MC4-R) agonist.

JKC363 TFA is a selective melanocortin MC4 receptor antagonist that exhibits a 90-fold higher affinity for the MC4 receptor (IC50=0.5 nM) compared to the MC3 receptor (44.9 nM). This compound effectively inhibits the α-MSH-induced stimulation of TRH release. It also demonstrates an anti-hyperalgesic effect [1] [2].

CCZ01048 TFA, an α-MSH analogue, demonstrates a strong binding affinity for the melanocortin 1 receptor (MC1R), displaying a K i value of 0.31 nM. It exhibits rapid internalization into B16F10 melanoma cells and maintains high in vivo stability. CCZ01048 TFA holds potential as an effective agent for PET imaging of malignant melanoma [1].