Melanocortin Receptor Antagonist

MC4R antagonist-3 is a benzimidazole or imidazopyridine derivative, as well as a MC4R antagonist with affinity for melanocortin receptors. MC4R antagonist-3 can be used in research related to inflammatory diseases, neuropathic pain, anxiety disorders, depressive disorders and skin diseases.

TCMCB07, 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.

MSG606 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 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.

Nonapeptide-1 (Melanostatine-5) acetate salt, a peptide hormone, is a selective antagonist of MC1R (K_i: 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.

HS024 is a selective MC4 receptor antagonist, with K_is of 0.29, 3.29, 5.45, 18.6 nM for MC4, MC5, MC3, and MC1, respectively. HS024 increase food intake.

SNT207858 free base is a selective, blood brain barrier penetrating, potent and orally active melanocortin-4 (MC-4) receptor antagonist. SNT207858 free base has an IC₅₀ of 22 nM (binding) and 11 nM (function) on the MC-4 receptor.

GPS1573 is a noncompetitive antagonist of melanocortin type 2 receptor (MC2R) that dose-dependently antagonizes ACTH-stimulated MC2R activity (IC₅₀=66 nM). GPS1573 can be used in the study of Cushing's disease due to its highly selective antagonism of MC2R.

PF-07258669 is an orally active melanocortin-4 receptor (MC4R) antagonist that antagonizes MC4R with an IC₅₀ of 13 nM (K_i=0.46 nM). PF-07258669 can be used for the research of cachexia, anorexia, or anorexia nervosa.

Nonapeptide-1 (Melanostatine-5), a peptide hormone, is a selective antagonist of MC1R (K_i: 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.

ML00253764 is a selective melanocortin receptor 4 (MC4R) antagonist, can induce apoptosis by inhibiting ERK1/2 and Akt phosphorylation, and has anticancer activity.

ACTH (11-24) is an adrenocorticotropic hormone (ACTH) receptor antagonist. ACTH (11-24) is a fragment of adrenocorticotropic and induces cortisol release. ACTH (11-24) can be used for the research of central nervous system.

TCMCB07 TFA, a cyclic nonapeptide peptide, is an orally active and brain-penetrant melanocortin receptor 4 (MC4R) antagonist. TCMCB07 TFA plays an important role in cachexia.

JKC363, a selective melanocortin MC4 receptor antagonist, has a 90-fold higher affinity at the MC4 receptor (IC₅₀=0.5 nM) than at the MC3 receptor (44.9 nM). JKC-363 blocks the stimulatory effect of α-MSH on TRH release. Anti-hyperalgesic effect.

PG106 TFA is a potent and selective human melanocortin 3 (hMC3) receptor antagonist (IC₅₀= 210 nM) and has noactivity at hMC4 receptors (EC₅₀=9900 nM) and hMC5 receptor.

MCL0020 is a potent and selective melanocortin MC4 receptor antagonist, with an IC₅₀ of 11.63 nM. MCL0020 dose-dependently and significantly attenuates restraint stress-induced anorexia without affecting food intake.

HS014 TFA is a potent and selective melanocortin-4 (MC4) receptor antagonist, with K_is of 3.16, 108, 54.4 and 694 nM for human MC4, MC1, MC3 and MC5 receptors respectively. HS014 TFA increases food intake in free-feeding rats.

ACTH (7-38) (human) is the 7-38 fragment of human ACTH (1-39). human ACTH (1-39), known as a corticotropin inhibitory peptide (CIP), is an antagonist of the ACTH receptor and has no any corticosteroid activity.

Undecylenoyl phenylalanine is an antagonist for α-melanocyte-stimulating hormone (MSH) and β-adrenergic receptor (β-ADR) to reduce the melanogenesis in melanocytes, reduces hyperpigmentation and thus ameliorates melasma lesions and solar lentigines.

Ac-c-Pro-Pro-Lys-Asp-NH2 is a selective human melanocortin 5 receptor (hMC5R) antagonist with an IC₅₀ of 10 nM.