melanocortin-4 receptor (mc4r)

[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.

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

MC-4R Agonist 1 is an agonist of the human melanocortin-4 receptor (MC-4R) and is useful in researching sexual dysfunction, obesity, and diabetes.

ML-00253764 hydrochloride is an antagonist of nonpeptidic melanocortin receptor 4 (MC4R) (Ki and IC50 of 0.16 µM and 0.103 µM, respectively).

PF-00446687 is a selective agonist of melanocortin-4 receptor (MC4R) (EC50 of 12 ± 1 nM).

Setmelanotide (RM-493) is a selective melanocortin-4 receptor agonist with EC50 values of 0.27 and 0.28 nM for human and rat MC4R. Setmelanotide enhances cAMP signaling, demonstrates functional selectivity, activates sympathetic preganglionic neurons to influence blood pressure, and is widely used to probe MC4R-MRAP2 interactions. Setmelanotide contributes to obesity-related research by modulating hunger and satiety circuits, reversing risperidone-induced weight gain in mice, and helping characterize MC4R variants in pediatric metabolic disorders. The anti-inflammatory actions of Setmelanotide in astrocytoma cells and the utility in combination with calorie restriction further highlight its broad value in metabolic and neuroendocrine research.

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).

MK-0493 is an effective and selective agonist of the melanocortin receptor 4 (MC4R). It also demonstrated significant reductions in energy intake.

MK-0493 is a novel, potent, and selective agonist for melanocortin receptor 4 (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)

Adrenocorticotropic Hormone (ACTH) (4-10), human is a potent agonist of the melanocortin receptor (MC4R).

Adrenocorticotropic Hormone (ACTH) (4-10) TFA (Acth (4-10)) is an agonist of potent melanocortin(MC4R) receptor .

Agouti-related Protein (AGRP) (83-132) Amide (human) is a segment derived from the agouti-related protein (AGRP), abundantly present in the hypothalamus' arcuate nucleus, and functions predominantly as an inverse agonist for the melanocortin-4 receptor (MC4R), thereby promoting food intake [1] [2].

α-MSH (MSH, amide) is amide stimulates melanocortin 1 receptor that results in the activation of adenylyl cyclase.

α-MSH acetate is an endogenous neuromodulatory peptide derived from POMC and an agonist of MC4R (melanocortin receptor 4). It inhibits food intake, fever, and inflammation, exhibiting multiple biological activities.

Bivamelagon (LB54640) is an orally effective MC4R (melanocortin 4) agonist with the advantage of crossing the blood-brain barrier, suitable for studying hypothalamic obesity and diabetes.

Ac-DArg-c[Cys-Glu-His-DPhe-Arg-Trp-Cys]-NH2 is a synthetic cyclic octapeptide acting as a melanocortin-4 receptor (MC4R) agonist, significantly elevating heart rate and blood pressure [1].

TCMCB07, a cyclic nonapeptide, serves as an orally active, brain-penetrant antagonist of the melanocortin receptor 4 (MC4R), with significant implications in the management of cachexia [1].

TCMCB07 acetate(1456699-27-6 Free base), a cyclic nonapeptide peptide, is an orally active and brain-penetrant melanocortin receptor 4 (MC4R) antagonist. TCMCB07 TFA plays an important role in cachexia.

TCMCB07 TFA is a cyclic nonapeptide and an orally active, brain-penetrating antagonist of the melanocortin receptor 4 (MC4R), playing a significant role in managing cachexia [1].

THIQ is a selective melanocortin-4 receptor (MC4R) agonist (hMC4R and rMC4R with IC50 of 1.2 nM and 0.6 nM , respectively).

(2R,2R)-PF-07258669' is an antagonist for the MC4R (melanocortin 4 receptor), primarily studied for its role in regulating appetite and energy expenditure.

MCL0020 is a potent and selective melanocortin MC4 receptor antagonist (IC50 values are 11.63, 1115, and >10,000 nM at MC4, MC3, and MC1 receptors, respectively). It significantly reverses stress-induced anorexia without affecting food intake in free-feeding rats and exhibits anxiolytic-like activity in vivo.

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.