MC1R
MC1R (Melanocortin 1 Receptor) is a melanocyte-enriched Gs-coupled receptor that functions as a central regulator of pigmentation, ultraviolet (UV) response, and melanoma susceptibility through control of melanin synthesis and cellular photoprotection[1]. Upon activation by melanocortin ligands such as α-melanocyte-stimulating hormone (α-MSH) or adrenocorticotropic hormone (ACTH), MC1R stimulates adenylate cyclase and elevates cAMP signaling, leading to activation of CREB and MITF and promoting eumelanin production, DNA repair, and antioxidant defense programs in melanocytes[2][3]. Mechanistically, MC1R signaling extends beyond pigmentation and contributes to adaptive responses against UV-induced genomic damage, linking melanogenesis with maintenance of genome stability[1][3]. In disease contexts, loss-of-function MC1R variants are associated with fair skin, red-hair phenotypes, impaired photoprotection, and increased melanoma risk, making MC1R a widely used genetic and experimental model for studying pigment biology and skin cancer susceptibility[1][2]. Compared with other melanocortin receptor family members, MC1R is distinguished by its predominant role in melanocyte biology and regulation of epidermal pigmentation, whereas other melanocortin receptors mediate endocrine, metabolic, or energy-homeostasis functions[4]. For experimental applications, both endogenous and synthetic MC1R agonists are used to investigate melanogenesis, DNA repair signaling, and photoprotective mechanisms, supporting continued interest in MC1R-targeted pharmacological studies[3][5].
References:
- [1]. Wolf Horrell EM, et al. Melanocortin 1 Receptor: Structure, Function, and Regulation. Front Genet. 2016 May 31;7:95. [Content Brief]
- [2]. Medicine-and-dentistry/melanocortin-1-receptor. sciencedirect.topics.
- [3]. Guida S, Guida G, Goding CR. MC1R Functions, Expression, and Implications for Targeted Therapy. J Invest Dermatol. 2022 Feb;142(2):293-302.e1. [Content Brief]
- [4]. Wikipedia.
- [5]. MC1R gene information from NCBI.
-
MC1R Related Products (18)
Related Products (18)
- 1
-
Melanotan I
0 ImagesSynonyms: MT-I; [Nle4,D-Phe7]-α-MSHMelanotan I (MT-I; [Nle4,D-Phe7]-α-MSH) is an α-MSH (HY-P0252) analog, synthetic melanotropic peptide, and melanocortin receptor (MCR) agonist. Melanotan I induces skin tanning by mimicking the action of α-MSH on the melanocortin 1 receptor (MC1R) in melanocytes. As an appetite suppressant, Melanotan I impairs the ability of insulin to inhibit endogenous glucose production, suppresses leptin secretion from adipose tissue, and thereby reduces voluntary feed intake in ewes. Melanotan I can be used in research related to UV-induced skin damage, polymorphic light eruption, ruminant feeding, and sexual dysfunction.
-
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).
-
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.
-
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.
-
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.
-
Palmitoyl tetrapeptide-20
0 ImagesCat. No.: HY-P5247Purity: 99.21%Synonyms: PTP20Palmitoyl tetrapeptide-20 (PTP20) is a biomimetic peptide agonist of α-MSH. Palmitoyl tetrapeptide-20 promotes hair pigmentation and delays hair graying by activating the MC1-R pathway (AC50: 0.16 nM), enhancing catalase activity to reduce H2O2 accumulation, and upregulating SIRT1 activity. Palmitoyl tetrapeptide-20 can be used in research on preventing hair loss and improving hair graying.
-
Nonapeptide-1
0 ImagesSynonyms: Melanostatine-5Nonapeptide-1 (Melanostatine-5), a peptide hormone, is a selective antagonist of MC1R (Ki: 40 nM). Nonapeptide-1 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 inhibits melanin synthesis, and can be used in the research of skin pigmentation and regulation of steroid production in the adrenal gland, skin cancer.
-
Resomelagon
0 ImagesSynonyms: AP1189Resomelagon (AP1189) is a potent, orally active melanocortin receptor (MR) agonist about MC1 and MC3. Resomelagon induces ERK1/2 phosphorylation and Ca2+ mobilization. Resomelagon has anti-inflammatory activity. Resomelagon can be used for obesity and chronic inflammation research.
-
CCZ01048 TFA
0 ImagesCat. No.: HY-P2336APurity: 98.54%CCZ01048 TFA, a α-MSH analogue, exhibits high binding affinity to melanocortin 1 receptor (MC1R) with a Ki of 0.31 nM. CCZ01048 TFA shows rapid internalization into B16F10 melanoma cells and high in vivo stability. CCZ01048 TFA is a promising candidate for PET imaging of malignant melanoma.
-
Setmelanotide monoacetate
0 ImagesSynonyms: RM-493 monoacetate; BIM-22493 monoacetate; IRC-022493 monoacetateSetmelanotide monoacetate (RM-493 monoacetate) is a blood-brain barrier-permeable, selective MC4R agonist with a Ki value of 2.1 nM for hMC4R. Setmelanotide monoacetate activates the CaMKK2/AMPK signaling pathway. Setmelanotide monoacetate mediates body weight homeostasis, feeding regulation and energy expenditure modulation; it reduces food intake, induces weight loss, decreases obesity severity, increases daytime activity and energy expenditure, lowers levels of leptin, triglycerides, fasting insulin and diastolic blood pressure, improves insulin sensitivity, glucose tolerance and fatty liver condition, and reverses respiratory depression. Setmelanotide monoacetate is applicable to research related to obesity, hyperinsulinemia, fatty liver and respiratory depression.
-
Melanotan I acetate
0 ImagesSynonyms: MT-I acetate; [Nle4,D-Phe7]-α-MSH acetateMelanotan I (MT-I; [Nle4,D-Phe7]-α-MSH) acetate is an α-MSH (HY-P0252) analog, synthetic melanotropic peptide, and melanocortin receptor (MCR) agonist. Melanotan I acetate induces skin tanning by mimicking the action of α-MSH on the melanocortin 1 receptor (MC1R) in melanocytes. As an appetite suppressant, Melanotan I acetate impairs the ability of insulin to inhibit endogenous glucose production, suppresses leptin secretion from adipose tissue, and thereby reduces voluntary feed intake in ewes. Melanotan I acetate can be used in research related to UV-induced skin damage, polymorphic light eruption, ruminant feeding, and sexual dysfunction.
-
hMC1R agonist 1
0 ImagesCat. No.: HY-P99004CAS No.: 3028881-87-7hMC1R agonist 1 is a selective hMC1R agonist. hMC1R agonist 1 activates adenylate cyclase to induce intracellular cAMP accumulation. hMC1R agonist 1 can be used for the research of immune-inflammatory disorders.
-
Palmitoyl tetrapeptide-20 TFA
0 ImagesCat. No.: HY-P5247ASynonyms: PTP20 TFAPalmitoyl tetrapeptide-20 (PTP20) TFA is a biomimetic peptide agonist of α-MSH. Palmitoyl tetrapeptide-20 TFA promotes hair pigmentation and delays hair graying by activating the MC1-R pathway (AC50: 0.16 nM), enhancing catalase activity to reduce H2O2 accumulation, and upregulating SIRT1 activity. Palmitoyl tetrapeptide-20 TFA can be used in research on preventing hair loss and improving hair graying.
-
RY764
0 ImagesCat. No.: HY-111131CAS No.: 491845-95-5RY746 is a selective MC4R agonist, with an EC50 of 10 nM. RY764 effectively inhibits food intake and reduces body weight gain in diet-induced obese (DIO) rat models. RY764 can be used for the study of obesity.
-
MSG606 TFA
0 ImagesCat. No.: HY-P1726AMSG606 TFA is a selective melanocortin 1 receptor (MC1R) antagonist. MSG606 TFA can abolish the neuroprotective effects of BMS-470539 (HY-15616) (MC1R agonist). MSG606 TFA can inhibit cancer cell proliferation and transition from the G1 to the S phase. MSG606 TFA can delay pain hypersensitivity and reduce cholesterol levels. MSG606 TFA can be used for the researches of cancer, inflammation, neurological and metabolic disease, such as breast cancer and subarachnoid hemorrhage (SAH).
-
(E/Z)-Resomelagon acetate
0 ImagesCat. No.: HY-168383CAS No.: 959850-74-9Synonyms: (E/Z)-AP1189 acetate(E/Z)-Resomelagon acetate is an agonist of melanocortin receptor 1 (MC1R) and MC3R with anti-inflammatory activities. (E/Z)-Resomelagon can be utilized in inflammation research.
-
CD08108
0 ImagesCat. No.: HY-125055ACAS No.: 1417342-67-6CD08108 is a selective MC1R full agonist with an EC50 of 70 nM against hMC1R. CD08108 participates in the melanogenesis process. CD08108 promotes cell proliferation. CD08108 can be used in studies related to vitiligo, subcutaneous diseases and photosensitive diseases.
- 1
