Catalog No.
Product Name
Application
Product Information
Citations
- Melanotan II is a high affinity melanocortin receptor agonist (Ki values are 0.67, 6.6, 34 and 46 nM for MC1, MC4, MC3 and MC5 receptors respectively).
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MC1R and MC5R antagonist
JNJ-10229570 is a novel MC1R and MC5R antagonist was used to treat primary human sebaceous cells. -
MC4R agonist
Setmelanotide (RM-493; BIM-22493; IRC-022493) is a selective melanocortin 4 receptor (MC4R) agonist with EC50s of 0.27 nM and 0.28 nM for human and rat MC4R, respectively.- Dajin Cho, .et al. , J Neurosci, 2023, Sep 6;43(36):6280-6296 PMID: 37591737
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MC4R agonist
PF-00446687 is a potent, selective melanocortin-4 receptor (MC4R) agonist with EC50 of 12????1 nM. Pf-446687 is brain penetrant. -
melanocortin receptor (MR) agonist
AP1189 is a biased agonist at receptors MC1 and MC3. AP1189 reduced cytokine release, an effect reliant on both MC1 and MC3 as evident from the use of Mc1r(-/-) and Mc3r(-/-) macrophages. - Bremelanotide Acetate (PT-141 Acetate), a synthetic peptide analogue of α-MSH, is an agonist at melanocortin receptors including the MC3R and MC4R for the treatment of sexual dysfunction.
- Melanotan 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 sunlight-induced skin cancers research.
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Pigmentation inhibitor
N,N′-Diferuloylputrescine acts as a pigment inhibitor, showing a 57% reduction in pigmentation. It also considerably diminishes the protein expression of MITF and displays potent antioxidant properties as a radical scavenger against reactive oxygen species.
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NSAID/COX inhibitor
Fenoprofen (LILLY-53858) is a nonsteroidal anti-inflammatory drug (NSAID) that functions primarily by inhibiting cyclooxygenase (COX) enzymes, thereby reducing the synthesis of pro-inflammatory prostaglandins. In addition to its classical NSAID activity, Fenoprofen has been identified as a positive allosteric modulator (PAM) of melanocortin receptors (MCRs), enhancing MCR-mediated signaling. Fenoprofen also promotes ERK1/2 activation in HEK293T cells, suggesting additional modulation of intracellular signaling pathways involved in inflammation and cellular proliferation. -
MC4R Agonist
Tetracosactide is a potent agonist of the melanocortin-4 receptor (MC4R), activating human MC4R with an EC50 of 0.65 nM. This synthetic analogue of adrenocorticotrophic hormone (ACTH) is known to stimulate the release of corticosteroids, including cortisol, from the adrenal gland. Tetracosactide is utilized in research investigating conditions such as ulcerative colitis, Crohn's disease, and various forms of arthritis, including juvenile and adult rheumatoid arthritis and osteoarthrosis. -
a-melanocyte Stimulating Hormone Analog
Modimelanotide is an α-melanocyte-stimulating hormone analog that exhibits high specificity for melanocortin receptors MCR1, MCR3, MCR4, and MCR5. This compound demonstrates notable anti-inflammatory and organ-protective properties, making it a valuable tool for research in conditions such as acute kidney injury. Investigating Modimelanotide can enhance understanding of melanocortin receptor signaling and its implications in various disease contexts. -
Melanogenesis Inhibitory Agent
Cadin-1(14)-ene-7a,11-diol is a sesquiterpene alcohol that functions as a melanogenesis inhibitory agent. It effectively suppresses melanin production in B16 melanoma cells stimulated by α-MSH, demonstrating potential application in skin-whitening treatments. This compound is valuable for research exploring mechanisms of pigmentation and therapies for hyperpigmentation disorders. -
MC4R Antagonist
TCMCB07 is a cyclic nonapeptide that functions as an antagonist of the melanocortin receptor 4 (MC4R). This compound demonstrates significant potential in the study of cachexia, exhibiting oral bioavailability and the ability to penetrate the blood-brain barrier. Its unique structure may also confer additional transport capabilities, making it a valuable tool in related research applications. -
MC-1 Receptor Agonist
BMS-470539 dihydrochloride is a selective agonist of the melanocortin-1 receptor (MC-1R), exhibiting an IC50 of 120 nM and an EC50 of 28 nM. This compound demonstrates potent anti-inflammatory properties while showing no activation of MC-3R and minimal partial agonism at MC-4R and MC-5R. BMS-470539 dihydrochloride is utilized in research focused on inflammatory conditions and the modulation of skin pigmentation. -
MC1R Agonist
Dersimelagon is a selective agonist of the melanocortin 1 receptor (MC1R) with demonstrated efficacy in human (EC50 of 8.16 nM), cynomolgus monkey (3.91 nM), mouse (1.14 nM), and rat (0.251 nM) models. It exhibits strong binding affinity for hMC1R and hMC4R, with Ki values of 2.26 nM and 32.9 nM, respectively. This compound is primarily utilized in research focused on skin pigmentation and the modulation of melanin synthesis. -
MC4R Agonist
Bivamelagon is a selective agonist of the melanocortin 4 receptor (MC4R) with an EC50 of 0.562 nM in a luciferase assay and 36.5 nM in a cAMP assay, demonstrating its potent activity. This compound exhibits a Ki value of 65 nM, indicating strong binding affinity to its target. Bivamelagon is valuable for research into metabolic disorders, particularly in the context of obesity and diabetes, providing insights into potential therapeutic applications. -
MC1R Antagonist
MSG606 is a selective antagonist of the melanocortin 1 receptor (MC1R), known for its ability to negate the neuroprotective effects of MC1R agonists. This compound effectively inhibits cancer cell proliferation and disrupts the transition from the G1 to S phase of the cell cycle. Additionally, MSG606 has demonstrated potential in delaying pain hypersensitivity and reducing cholesterol levels. It is valuable for research applications related to cancer, inflammation, neurological disorders, and metabolic diseases, including breast cancer and subarachnoid hemorrhage. -
Melanocortin Receptor Agonist
Adrenocorticotropic Hormone (ACTH) (1-39), human is a potent melanocortin receptor agonist. It plays a critical role in stimulating cortisol release from the adrenal cortex and is involved in regulating stress responses, metabolism, and immune function. This peptide can be utilized in research focusing on adrenal function, neuroendocrine regulation, and related therapeutic studies. -
MC4R Agonist
α-MSH TFA is a potent agonist of the melanocortin receptor 4 (MC4R). This endogenous neuropeptide exhibits anti-inflammatory and antipyretic properties, making it valuable for research into metabolic regulation and neuroinflammatory responses. As a post-translational derivative of pro-opiomelanocortin (POMC), α-MSH TFA serves as an important tool for studying the physiological roles of melanocortins in various biological processes. -
MC4R Agonist
MK-0493 is an orally active agonist of the melanocortin-4 receptor (MC4R), known for its role in regulating appetite and energy balance. This compound is demonstrated to reduce food intake and suppress weight gain, while also elevating blood pressure at elevated doses. Additionally, MK-0493 displays preclinical activity in erectile function regulation, making it a valuable tool in obesity and metabolic disorder research. -
Melanocortin Receptor Agonist
Adrenocorticotropic hormone (1-39), rat is a potent agonist of the melanocortin 2 (MC2) receptor. This peptide is crucial in regulating adrenal steroidogenesis and is significant for research in stress response and metabolism. Its use in studies can provide valuable insights into the functioning of the hypothalamic-pituitary-adrenal (HPA) axis and related endocrine disorders. -
MC4-R Agonist
β-Melanocyte Stimulating Hormone (MSH), human, is a 22-residue peptide that functions as an endogenous agonist of the melanocortin-4 receptor (MC4-R). It plays a critical role in regulating energy homeostasis, appetite, and body weight. This compound is valuable for research applications focused on metabolic disorders, obesity, and neurobiology. -
Melanocortin Receptor Agonist
Bremelanotide is a potent melanocortin receptor agonist that primarily targets the MC4R. It is known to enhance dopamine release, leading to the modulation of appetitive sexual behaviors, including female mounting behavior and repetitive self-grooming. This compound is valuable for investigating hypoactive sexual desire disorders and understanding the neurobiological mechanisms underlying sexual arousal and motivation. -
Melanocortin Receptor Antagonist
SNT-207858 free base is a selective melanocortin-4 (MC-4) receptor antagonist that effectively penetrates the blood-brain barrier. With an IC50 of 22 nM for binding and 11 nM for functional inhibition, this compound demonstrates potent activity against the MC-4 receptor. It is a valuable tool for research applications focused on understanding melanocortin signaling pathways and their implications in neurological and metabolic disorders. -
MC4 Antagonist
PF-07258669 is a potent orally active antagonist of the melanocortin-4 receptor (MC4R), displaying an IC50 of 13 nM and a Ki of 0.46 nM. This compound has significant implications for research into conditions related to cachexia, anorexia, and anorexia nervosa, making it a valuable tool for studying the regulatory mechanisms of appetite and energy homeostasis. -
MC4R Antagonist
ML-00253764 hydrochloride is a nonpeptidic antagonist of the melanocortin receptor 4 (MC4R), demonstrating a Ki of 0.16 μM and an IC50 of 0.103 μM. This compound effectively penetrates the blood-brain barrier, making it suitable for central nervous system studies. Its antagonistic activity at MC4R suggests potential applications in obesity research and metabolic disorder investigations. -
Melanocortin Receptor Agonist
Resomelagon is a potent orally active melanocortin receptor agonist, primarily targeting MC1 and MC3. This compound induces ERK1/2 phosphorylation and promotes calcium mobilization, showcasing significant anti-inflammatory properties. Resomelagon is predominantly employed in research focused on obesity and chronic inflammation, providing valuable insights into metabolic and inflammatory pathways. -
Melanocortin 4 Receptor Agonist
RO27-3225 TFA is a selective agonist of the melanocortin 4 receptor (MC4R), exhibiting an EC50 of 1 nM for MC4R and 8 nM for MC1R, demonstrating approximately 30-fold selectivity for MC4R over MC3R. This compound is recognized for its neuroprotective and anti-inflammatory properties, making it valuable in research related to metabolic regulation and inflammatory conditions. RO27-3225 TFA is suitable for studies focused on the role of MC4R in various physiological and pathological processes. -
MC2R Antagonist
GPS1573 is a noncompetitive antagonist of the melanocortin type 2 receptor (MC2R), exhibiting dose-dependent inhibition of adrenocorticotropic hormone (ACTH)-induced MC2R activity with an IC50 value of 66 nM. This compound is particularly valuable in research focused on Cushing's disease, given its high selectivity for MC2R antagonism. Its properties make GPS1573 an important tool for studying adrenal regulation and related endocrine disorders. -
MC3 Receptor Agonist
γ1-MSH is an agonist of the melanocortin MC3 receptor, exhibiting a Ki of 34 nM for the rat MC3 receptor. This compound demonstrates approximately 40-fold selectivity over the MC4 receptor, with a Ki of 1318 nM. γ1-MSH is valuable for research applications exploring the role of melanocortin receptors in metabolic processes and neuroendocrine regulation. -
MC4R Agonist
MK-0493 hydrochloride is a selective agonist of the melanocortin receptor 4 (MC4R), known for its potent and orally active properties. It has been shown to effectively reduce energy intake, making it a valuable tool for research in metabolic disorders and obesity. Its targeted mechanism of action facilitates the exploration of MC4R pathways in various biological studies. -
Melanocortin Receptor Agonist
Adrenocorticotropic Hormone (ACTH) (4-10), human is a potent agonist of the melanocortin 4 receptor (MC4R). This peptide fragment is involved in the regulation of various physiological processes, including appetite control and energy homeostasis. Its applications extend to research in metabolic disorders, obesity, and neuroendocrine function, offering insights into MC4R signaling pathways. -
ACTH Fragment
ACTH (22-39) is a fragment of adrenocorticotropic hormone (ACTH), specifically encompassing the amino acid sequence from 22 to 39. This peptide retains important biological activity relating to the stimulation of adrenal steroidogenesis, making it valuable for research in endocrinology and stress response studies. It is commonly utilized in investigations of the hypothalamic-pituitary-adrenal (HPA) axis and the mechanisms underlying adrenal function. -
MC4R Antagonist
ML00253764 is a selective antagonist of the melanocortin receptor 4 (MC4R). It induces apoptosis through the inhibition of ERK1/2 and Akt phosphorylation pathways, demonstrating notable anticancer activity. This compound is valuable for research focused on cancer biology and the modulation of melanocortin signaling pathways. -
MC3 Agonist
[D-Trp8]-γ-MSH is a selective agonist of the melanocortin 3 (MC3) receptor, exhibiting an IC50 of 6.7 nM in CHO cells. This compound also demonstrates activity against the MC4 and MC5 receptors, with IC50 values of 600 nM and 340 nM, respectively. [D-Trp8]-γ-MSH is implicated in research applications related to inflammatory disorders, showing potential neuroprotective effects in conditions such as rheumatoid arthritis and colitis. -
ACTH Analogue
(D-Ser1)-ACTH (1-24) is an analogue of adrenocorticotropic hormone (ACTH) that retains the critical biological activities associated with ACTH signaling. This peptide exhibits potent effects on cortisol secretion and adrenal cortex stimulation, making it valuable in research related to stress response, adrenal function, and endocrinology. It is suitable for studies involving various model organisms, including human, bovine, mouse, ovine, porcine, rabbit, and rat. -
ACTH Fragment
ACTH (1-16) (human) is a fragment of the adrenocorticotropic hormone that primarily targets the ACTH receptor. This peptide has been shown to enhance cardiovascular function and improve survival rates in models of experimental hemorrhagic shock. It serves as a valuable tool in research applications focused on stress response and the physiological mechanisms underlying shock and related cardiovascular conditions. -
ACTH Receptor Antagonist
ACTH (11-24) is an adrenocorticotropic hormone (ACTH) receptor antagonist that modulates cortisol release through the inhibition of ACTH receptors. This peptide fragment serves as a valuable tool for investigating endocrine regulation and its effects within the central nervous system. ACTH (11-24) is particularly useful in studies related to stress response, neuroendocrine function, and potential therapeutic applications in disorders linked to ACTH signaling. -
ACTH Receptor Antagonist
ACTH (7-38) (human) is a fragment of human adrenocorticotropic hormone (ACTH) that acts as an antagonist at the ACTH receptor. It functions as a corticotropin inhibitory peptide (CIP) and exhibits no corticosteroid activity. This reagent is useful for studies investigating adrenal function, stress response mechanisms, and the regulation of steroid hormone production. -
MC4R Agonist
Setmelanotide monoacetate is a potent agonist of the melanocortin 4 receptor (MC4R), exhibiting EC50 values of 0.27 nM in human and 0.28 nM in rat models. This compound plays a crucial role in regulating appetite and energy homeostasis, making it valuable for research applications related to obesity and metabolic disorders. Its specificity for MC4R also makes it a useful tool for studying melanocortin signaling pathways. -
Melanocortin 4 Receptor Agonist
PG-931 is a potent agonist of the melanocortin 4 receptor (MC4R), exhibiting an IC50 of 0.58 nM, while demonstrating selective activity against the human MC3R and MC5R with IC50 values of 55 nM and 2.4 nM, respectively. This compound has shown significant biological activity in reversing haemorrhagic shock and mitigating multiple organ damage in vivo. PG-931 is valuable for research applications focused on obesity, metabolic disorders, and neurodegenerative diseases involving melanocortin signaling pathways. -
Melanocortin Receptor Agonist
Resomelagon acetate is a potent, orally active melanocortin receptor (MC) agonist, primarily targeting MC1 and MC3 receptors. It effectively induces ERK1/2 phosphorylation and promotes calcium mobilization, contributing to its anti-inflammatory properties. This compound is particularly relevant for research focused on obesity and chronic inflammation. -
MC4 Receptor Antagonist
HS024 is a selective antagonist of the melanocortin-4 (MC4) receptor, exhibiting inhibition constants (Kis) of 0.29 nM for MC4, 3.29 nM for MC5, 5.45 nM for MC3, and 18.6 nM for MC1. This compound is notable for its ability to enhance food intake, making it a valuable tool for research in metabolic disorders, appetite regulation, and obesity studies. HS024 may facilitate the exploration of pathways related to energy homeostasis and weight management. -
hMC1R Agonist
hMC1R Agonist 1 selectively activates the human melanocortin 1 receptor (hMC1R) with an EC50 of 3 nM. This compound demonstrates over 300-fold selectivity for hMC1R compared to hMC3R, hMC4R, and hMC5R, which have significantly higher EC50 values (902 nM, 915 nM, and >1000 nM, respectively). hMC1R Agonist 1 holds promise for potential therapeutic applications within the melanocortin receptor family, particularly in conditions related to pigmentation and metabolic regulation. -
Melanogenesis Inhibitor
(-)-Isodocarpin is a diterpenoid that acts as a potent melanogenesis inhibitor, exhibiting an IC50 of 0.19 μM in B16 4A5 cell lines. This compound effectively suppresses the expression of key melanogenic enzymes, including tyrosinase, tyrosine-related protein (TRP)-1, and TRP-2 mRNA. (-)-Isodocarpin is valuable for research applications focused on skin pigmentation, melanin synthesis, and related dermatological studies. -
Adrenocorticotropin Hormone Fragment
ACTH (4-11) is a fragment of the adrenocorticotropin hormone that primarily interacts with melanocortin receptors, exhibiting mild α-melanocyte stimulating hormone (α-MSH) activity at elevated concentrations of 100 and 1000 nM. This compound is utilized in research applications focused on the regulation of stress responses and the study of melanocortin receptor signaling pathways. Its unique properties make it a valuable tool in investigations of physiological processes related to adrenal function and pigment regulation. -
MC4R Agonist
MC4-NN2-0453 is a selective agonist of the melanocortin 4 receptor (MC4R) and serves as an analog of alpha-melanocyte-stimulating hormone (α-MSH). This compound is particularly relevant in the study of obesity, as it stimulates MC4R activity, which is known to play a crucial role in regulating appetite and energy expenditure. Its application in obesity research allows for better understanding of mechanisms that could lead to novel therapeutic strategies.
