Melanocortin Receptor

Cat. No.

A16876

CAS No.

524923-88-4

JNJ-10229570

Synonyms: UNII-N9IX402L35

JNJ-10229570 is a novel MC1R and MC5R antagonist was used to treat primary human sebaceous cells.

Cat. No.

A22734

CAS No.

168482-23-3

SHU 9119

SHU 9119 is a potent human melanocortin 3 and 4 receptors (MC3/4R) antagonist and a partial MC5R agonist; with IC50 values of 0.23, 0.06, and 0.09 nM for human MC3R, MC4R and MC5R, respectively.

Cat. No.

A61627

CAS No.

1456699-27-6

TCMCB07

Synonyms: Mifomelatide

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.

Cat. No.

A61631

CAS No.

1416983-77-1

MSG606

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.

Cat. No.

A61639

CAS No.

1104662-66-9

SNT-207858 free base

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.

Cat. No.

A61640

CAS No.

2755890-53-8

PF-07258669

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.

Cat. No.

A61641

CAS No.

1706524-94-8

ML-00253764 hydrochloride

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.

Cat. No.

A61644

CAS No.

2445822-54-6

GPS1573

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.

Cat. No.

A61650

CAS No.

681847-92-7

ML00253764

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.

Cat. No.

A61655

CAS No.

4237-93-8

ACTH (11-24)

Synonyms: Adrenocorticotropic Hormone (11-24)

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.

Cat. No.

A61656

CAS No.

68563-24-6

ACTH (7-38) (human)

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.

Cat. No.

A61661

CAS No.

212370-59-7

HS024

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.

Cat. No.

A61667

CAS No.

2755890-68-5

(2R,2R)-PF-07258669

(2R,2R)-PF-07258669 is an antagonist of the melanocortin 4 receptor (MC4R). It serves as a valuable tool in research aimed at understanding the regulation of appetite and energy expenditure. Its application can aid in elucidating the role of MC4R in metabolic processes and potential therapeutic interventions for obesity and related disorders.

Cat. No.

A61677

CAS No.

207678-81-7

HS014

HS014 is a selective antagonist of the melanocortin-4 (MC4) receptor, exhibiting a Ki of 3.16 nM for human MC4, while demonstrating significantly lower affinities for MC1, MC3, and MC5 receptors. This compound has been shown to modulate morphine-induced behaviors in murine models, as well as to facilitate increased food intake in free-feeding rat studies. HS014 is a valuable tool in research exploring the regulation of appetite and pain modulation.

Cat. No.

A61678

CAS No.

944111-22-2

PG106

PG106 is a selective antagonist of the human melanocortin 3 (hMC3) receptor, exhibiting a potency with an IC50 of 210 nM. The compound demonstrates significant specificity, showing minimal activity at the hMC4 receptor (EC50 of 9900 nM) and no interaction with the hMC5 receptor. Research applications include studies focused on metabolic regulation and potential therapeutic targets related to obesity and related disorders.

Cat. No.

A61680

CAS No.

768357-45-5

MCL-0129

MCL-0129 is a selective antagonist of the melanocortin 4 receptor (MC4R), known for its potential anxiolytic and antidepressant properties. This compound exhibits significant anxiolytic and antidepressant-like effects in various rodent models, making it a valuable tool for research into neuropsychiatric disorders. Its specific targeting of MC4R supports studies aimed at elucidating the mechanisms of action in stress-related and mood disorders.

Cat. No.

A61692

CAS No.

159600-82-5

(p-Iodo-Phe7)-ACTH (4-10)

(p-Iodo-Phe7)-ACTH (4-10) is a derivative of adrenocorticotrophic hormone (ACTH) that functions as a melanocortin receptor antagonist. This compound effectively inhibits the action of α-melanocyte-stimulating hormone (α-MSH), thereby reducing excessive grooming behavior observed in rat models. It serves as a valuable tool in research focused on the modulation of melanocortin signaling pathways and behaviors influenced by the central nervous system.

Cat. No.

A61706

CAS No.

596135-92-1

Ac-c[Cys-Glu-His-d-Phe-Arg-Trp-d-Cys]-Pro-Pro-Lys-Asp-NH2

Ac-c[Cys-Glu-His-d-Phe-Arg-Trp-d-Cys]-Pro-Pro-Lys-Asp-NH2 is a selective antagonist of the human melanocortin 5 receptor (hMC5R), exhibiting an IC50 value of 10 nM. This compound is crucial for studies focusing on hMC5R-related signaling pathways and their implications in various physiological processes. Its specificity makes it a valuable tool for investigating the role of hMC5R in metabolic regulation and other biological functions.

Cat. No.

A61713

CAS No.

884538-31-2

MPCI

MPCI is a selective antagonist of the melanocortin-4 receptor (MC4R), exhibiting pharmacological chaperone activity. With a Ki value of 0.218 μM determined in HEK293 cells expressing human MC4R, MPCI is valuable in researching the mechanisms underlying MC4R-deficient obesity. This compound can facilitate studies on metabolic regulation and potential therapeutic approaches for related disorders.