melanocortin-1 receptor

Dersimelagon (MT-7117) is an orally active, selective melanocortin 1 receptor (MC1R) agonist with EC50 values ​​of 8.16, 3.91, 1.14, and 0.251 nM for human (h), cynomolgus monkey (cm), mouse (m), and rat (r) MC1R, respectively. Dersimelagon exhibits good affinity for hMC1R and hMC4R, with Ki values ​​of 2.26 and 32.9 nM, respectively. Dersimelagon can be used in the study of skin pigmentation[1].

BMS-470539 dihydrochloride is a selective and highly potent melanocortin 1 receptor (MC-1 R) agonist with anti-inflammatory activity. BMS-470539 attenuates oxidative stress and neuronal apoptosis via the MC1R/cAMP/PKA/Nurr1 signaling pathway in a neonatal hypoxia-ischemia rat model.

JNJ-10229570 (UNII-N9IX402L35) is an antagonist of melanocortin receptor 1 (MC1R) and melanocortin receptor 5 (MC5R), which inhibits sebaceous gland differentiation and the production of sebum-specific lipids.

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

AP1189 acetate is a biased agonist at melanocortin 1 and melanocortin 3 receptors.

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

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.

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

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

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)

Resomelagon (AP1189) is a potent, orally active melanocortin receptor (MR) agonist that induces Ca2+ mobilization and ERK1/2 phosphorylation, demonstrating anti-inflammatory activity useful in obesity and chronic inflammation research [1] [2].

Dersimelagon phosphate is a selective melanocortin-1 receptor (MC1R) agonist that increases skin melanin without sun exposure and is being developed to increase light tolerance in EPP/XLP patients.

RO27-3225, also known as RO273225 is a melanocortin type 4 receptor agonist with EC50 = 1 nM. It may alleviate intestinal dysfuntion and brain damage. It has been investigated for an anti-obesity medication. Ro 27-3225 shows some activity at the MC1 receptor. Ro 27-3225 reverses hemorrhagic shock, reduces multiple organ damage, and improves survival.

Melanotan II acetate is an agonist of melanocortin receptor 1 (MC1R), MC3R, MC4R, and MC5R. It has been shown to improve recovery of sciatic nerve function after mechanical injury and increase cisplatin-induced decreases in sensory nerve conduction velocity. Melanotan II acetate increases oxygen consumption and protein levels of uncoupling protein 1 (UCP1) in brown adipose tissue homogenates and decreases food intake, body weight, and serum levels of leptin, glucose, insulin, and cholesterol.

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].

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].

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].

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].

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].