- Signaling Pathways
- GPCR/G Protein Neuronal Signaling
- Melanocortin Receptor
Melanocortin Receptor
MC Receptor
The melanocortin (MC) receptors represent a subfamily of G-protein-coupled receptors (GPCRs) where the different subtypes are involved in a wide range of physiological functions such as pigmentation, steroid secretion, energy homeostasis, and food intake. The melanocortin receptor (MCR) family consists of five G-protein-coupled receptors (MC1R-MC5R). MC1R controls pigmentation, MC2R is a critical component of the hypothalamic-pituitary-adrenal axis, MC3R and MC4R have a vital role in energy homeostasis and MC5R is involved in exocrine function.
MCRs are activated by a variety of neuropeptides, termed melanocortins, that include the adrenocorticotropic hormone (ACTH) andα, β and γ-melanocyte-stimulating hormones (MSHs). Melanocortins derive from post-translational processing of the common polypeptide precursor pro-opiomelanocortin, expressed mainly in the hypothalamus and pituitary.
Melanocortin Receptor Isoform Specific Products
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Melanocortin Receptor Inhibitors
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Melanocortin Receptor Agonists
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Melanocortin Receptor Antagonists
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Melanocortin Receptor Activators
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Melanocortin Receptor Modulators
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Melanocortin Receptor Inducer
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Melanocortin Receptor Degrader
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Melanocortin Receptor Controls
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Melanocortin Receptor Ligands
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Melanocortin Receptor Related Products (182)
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Antibodies (2)
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Melanocortin Receptor Isoform Comparison
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α-MSH
0 Imagesα-MSH (α-Melanocyte-Stimulating Hormone), an endogenous neuropeptide, is an endogenous melanocortin receptor 4 (MC4R) agonist with anti-inflammatory and antipyretic activities. α-MSH is a post-translational derivative of pro-opiomelanocortin (POMC). -
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Setmelanotide
0 ImagesSynonyms: RM-493; BIM-22493; IRC-022493 -
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Eriodictyol
0 ImagesEriodictyol ((±)-Huazhongilexone; Dihydroluteolin) is an orally active TRPV1 receptor antagonist (IC50=44-47 nM, rTRPV1) with antioxidant and anti-inflammatory activities. Eriodictyol effectively inhibits lipid peroxidation and the release of proinflammatory cytokines by specifically antagonizing the TRPV1 receptor and activating the Nrf2 signaling pathway. Eriodictyol reduces the levels of ICAM-1, VEGF, eNOS and TNF-α in the retina and maintains the integrity of the blood-retinal barrier. Eriodictyol alleviates oxidative stress-induced apoptosis and hyperalgesia, enhances the activity and cytotoxicity of immune cells (such as B lymphocytes, NK cells and macrophages), and increases the levels of antioxidant enzymes simultaneously. Eriodictyol can be used in the research of diabetic retinopathy, acute lung injury and various pain-related diseases. -
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Melanotan I
0 ImagesSynonyms: MT-I; [Nle4,D-Phe7]-α-MSHMelanotan I is a potent non-selective melanocortin receptor (MCR) agonist. Melanotan I is a synthetic analogue of α-melanocyte stimulating hormone (α-MSH) that stimulates melanogenesis. Melanotan I can induce skin tanning by mimicking the actions of a-MSH on the melanocortin type 1 receptors (MC1R) of melanocytes. Melanotan I can be used for the research of sun-induced skin cancer, melanoma, inflammation and male erectile dysfunction. -
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Melanotan (MT)-II
0 ImagesMelanotan (MT)-II is a melanocortin receptor agonist. Melanotan (MT)-II activates melanocortin receptor 3 and melanocortin receptor 4, and stimulates the release of central endogenous oxytocin. Melanotan (MT)-II reverses recognition memory impairment, increased anxiety levels and reduced exploratory tendency in zebrafish exposed to short-term high-fat diet. Melanotan (MT)-II improves impaired social behavior indicators in mouse models of autism spectrum disorder. Melanotan (MT)-II induces weight loss, reduces food intake and exerts anorectic effects. Melanotan (MT)-II increases intracavernous pressure and erectile activity in brown rats. Melanotan (MT)-II can be used in studies related to memory impairment, anxiety, reduced exploratory behavior, autism spectrum disorder, obesity and erectile dysfunction. -
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PG-901
0 ImagesPG-901 is a full, selective MC5R agonist (EC50 = 0.072 nM for hMC5R). PG-901 is also a full antagonist at the hMC3R and the hMC4R (Kb: 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. -
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Modimelanotide acetate
0 ImagesCat. No.: HY-105305ASynonyms: ABT-719 acetate; AP-214 acetateModimelanotide (ABT-719) acetate is an α-melanocyte-stimulating hormone analog. Modimelanotide acetate has high specific binding ability to melanocortin receptors (MCR1, 3, 4, 5). Modimelanotide acetate possesses anti-inflammatory and organ-protective effects. Modimelanotide acetate can be used in the research of diseases such as acute kidney injury. -
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PRAME peptide (425-433) acetate
0 ImagesCat. No.: HY-P11280APurity: 98.16%PRAME peptide (425-433) acetate is a proteasome-degraded peptide derived from the cancer-testis antigen PRAME (Preferentially Expressed Antigen in Melanoma). PRAME peptide (425-433) acetate is restricted by HLA-A*02:01 and can serve as a target for bispecific T cell engager therapy in the context of major histocompatibility complex I presentation. PRAME peptide (425-433) acetate shows application potential in various malignant tumors and is widely suitable for research related to solid tumors, melanoma, ovarian cancer, endometrial cancer, and lung cancer (including lung adenocarcinoma and lung squamous cell carcinoma). PRAME peptide (425-433) acetate can be used to explore disease of triple-negative breast cancer, diffuse large B-cell lymphoma, and head and neck squamous cell carcinoma. -
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THIQ
0 ImagesTHIQ is the first selective agonist of the melanocortin-4 receptor (MC4R), with high affinity and potency for hMC4R (IC50=1.2 nM, EC50=2.1 nM) and rMC4R (IC50=0.6 nM, EC50=2.9 nM). THIQ maintains low potency at MC1R, MC3R and MC5R. THIQ plays a role in eliciting erectile activity in rodents. THIQ acts as a pharmacoperone of the MC4R rescuing the cell surface expression and signaling of some intracellularly retained MC4R mutants. -
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- SHU 9119
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Bremelanotide Acetate
0 ImagesSynonyms: PT-141 AcetateBremelanotide (PT-141) Acetate is a melanocortin receptor agonist. Bremelanotide Acetate can activate MC4R and increases dopamine release. Bremelanotide Acetate induces appetitive sexual behaviors, female mounting behavior, and repetitive self-grooming. Bremelanotide Acetate can be used for the research of hypoactive sexual desire disorders. -
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TCMCB07
0 ImagesSynonyms: MifomelatideTCMCB07, a cyclic nonapeptide peptide, is an orally active and brain-penetrant melanocortin receptor 4 (MC4R) antagonist. TCMCB07 plays an important role in cachexia. TCMCB07 has potential transport capabilities. -
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Adrenocorticotropic Hormone (ACTH) (1-39), human
0 ImagesSynonyms: 1-39-Corticotropin (human)Adrenocorticotropic Hormone (ACTH) (1-39), human is a melanocortin receptor agonist. -
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- Bivamelagon
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Dersimelagon
0 ImagesSynonyms: MT-7117Dersimelagon (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 shows good affinity for hMC1R and hMC4R with Ki values of 2.26, 32.9 nM, respectively. Dersimelagon can be used for the research of skin pigmentation. -
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MSG606
0 ImagesMSG606 is a selective melanocortin 1 receptor (MC1R) antagonist. MSG606 can abolish the neuroprotective effects of BMS-470539 (HY-15616) (MC1R agonist). MSG606 can inhibit cancer cell proliferation and transition from the G1 to the S phase. MSG606 can delay pain hypersensitivity and reduce cholesterol levels. MSG606 can be used for the researches of cancer, inflammation, neurological and metabolic disease, such as breast cancer and subarachnoid hemorrhage (SAH). -
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JNJ-10229570
0 ImagesJNJ-10229570 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. JNJ-10229570 inhibits the binding of 125I-NDP-α-MSH to cells expressing human MC1R and MC5R, with IC50 values of 270 nM and 200 nM, respectively. -
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- PF-00446687 free base
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BMS-470539 dihydrochloride
0 ImagesBMS-470539 dihydrochloride is a highly potent and selective melanocortin-1 receptor (MC-1R) agonist with an IC50 of 120 nM, an EC50 of 28 nM. BMS-470539 dihydrochloride does not activate MC-3R and is a very weak partial agonist at MC-4R and MC-5R. BMS-470539 dihydrochloride has potently anti-inflammatory properties. -
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Nonapeptide-1 acetate salt
0 ImagesCat. No.: HY-P0097ASynonyms: Melanostatine-5 acetate saltNonapeptide-1 (Melanostatine-5) acetate salt, a peptide hormone, is a selective antagonist of MC1R (Ki: 40 nM). Nonapeptide-1 acetate salt is a competitive α-MSH antagonist that potently inhibits intracellular cAMP and melanosome dispersion induced by α-MSH in melanocytes (IC50: 2.5 nM and 11 nM, respectively). Nonapeptide-1 acetate salt inhibits melanin synthesis, and can be used in the research of skin pigmentation and regulation of steroid production in the adrenal gland, skin cancer. -
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