melanocortin

HS024 is a highly potent melanocortin MC4 receptor antagonist (Ki values are 0.29, 18.6, 5.45 and 3.29 nM for cloned human MC4, MC1, MC3 and MC5 receptors respectively). Increases food intake, and blocks α-MSH- and MTII-induced hypotension and bradycardia in rats, following central administration in vivo.

ACTH (1-17) acetate is a potent agonist at the human melanocortin 1 (MC1) receptor with high affinity(Ki = 0.21 nM).

[D-Trp8]-γ-MSH acetate(321351-81-9 free base) is a selective melanocortin 3 (MC3) receptor agonist (IC50 values are 6.7, 340 and 600 nM for human MC3, MC5 and MC4 receptors respectively) and displays anti-inflammatory efficacy.

PG 106 acetate is an effective and selective antagonist of the human melanocortin 3 (hMC3) receptor with an IC50 of 210 nM. PG 106 acetate has no activity with the hMC5 receptor and hMC4 receptors with an EC50 of 9900 nM.

HS 014 acetate is a potent and selective melanocortin MC4 receptor antagonist (Ki values are 3.16, 108, 54.4 and 694 nM for cloned human MC4, MC1, MC3 and MC5 receptors respectively). Increases food intake in rats and nociception in mice following central

Adrenocorticotropic Hormone (ACTH) (1-39), rat (TFA), is a potent agonist of the melanocortin 2 receptor (MC2).

Setmelanotide (BIM-22493) is a selective agonist of melanocortin 4 receptor (MC4R)(human and rat MC4R with EC50s of 0.27 nM and 0.28 nM, respectively).

Setmelanotide Acetate(920014-72-8 free base) (RM-493 Acetate) is a selective agonist of melanocortin 4 receptor (MC4R)(human and rat MC4R with EC50s of 0.27 nM and 0.28 nM, respectively).

SHU 9119 is an effective human melanocortin 3 and 4 receptors (MC3/4R) antagonist and a partial MC5R agonist (IC50: 0.23, 0.06, and 0.09 nM for human MC3R, MC4R and MC5R, respectively).

SHU 9119 acetate is a well-known antagonist of human melanocortin 3 and 4 (hMC3R, hMC4R) receptors and a partial hMC5R agonist. The IC50 values of human MC3R, MC4R and MC5R is 0.23, 0.06, and 0.09 nM respectively.

Bremelanotide is a synthetic peptide analog of alpha-MSH and is an agonist at melanocortin receptors including the MC3R and MC4R.

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)

Nonapeptide-1 (Melanostatine-5) acetate salt is a peptide hormone that functions as a selective and competitive antagonist of the melanocortin 1 receptor (MC1R) with a binding affinity (K i) of 40 nM. It effectively inhibits α-MSH-induced increases in intracellular cyclic AMP (cAMP) and melanosome dispersion in melanocytes, with inhibitory concentrations (IC 50) of 2.5 nM and 11 nM, respectively. By inhibiting melanin synthesis, Nonapeptide-1 acetate salt is used in research related to skin pigmentation, adrenal gland steroid production regulation, and skin cancer [1] [2] [3].

PG-931 TFA, a potent and selective agonist of the melanocortin 4 (MC4) receptor (IC50=0.58 nM) compared to the hMC3R (IC50=55 nM) and hMC5R (IC50=2.4 nM), is an analog of SHU 9119. This compound has demonstrated efficacy in reversing hemorrhagic shock and preventing multiple organ damage in vivo [2].

PG106 TFA is a potent, selective antagonist of the human melanocortin 3 (hMC3) receptor, displaying an IC50 value of 210 nM, while exhibiting negligible activity at the hMC4 receptors (EC50 = 9900 nM) and hMC5 receptor [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].

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].

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].

HS014 TFA, a potent and selective antagonist of the melanocortin-4 (MC4) receptor, exhibits K i values of 3.16, 108, 54.4, and 694 nM for the human MC4, MC1, MC3, and MC5 receptors, respectively. It effectively increases food intake in free-feeding rats [1] [2].

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

Afamelanotide acetate is a synthetic α-melanocyte stimulating hormone analogue and first-in-class melanocortin-1 receptor agonist, used to for Erythropoietic Protoporphyria.

γ-1-Melanocyte Stimulating Hormone (MSH), amide, an 11-amino acid peptide, plays a critical role in regulating sodium (Na+) balance and blood pressure by activating melanocortin receptor 3 (MC3-R).

ACTH (1-17) TFA, an analogue of adrenocorticotropin, is a potent agonist for the human melanocortin 1 (MC1) receptor with a dissociation constant (K i) of 0.21 nM.

CCZ01048, an analogue of α-melanocyte-stimulating hormone (α-MSH), demonstrates a high binding affinity for the melanocortin 1 receptor (MC1R), with a Ki of 0.31 nM. It rapidly internalizes into B16F10 melanoma cells and exhibits notable in vivo stability, making it a promising candidate for PET imaging of malignant melanoma [1].