MC4R 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.

MC4R antagonist-2 is a potent melanocortin 4 receptor (MC4R) antagonist with an IC₅₀ of 0.54 nM. MC4R antagonist-2 can be used for the research of MC4R-mediated conditions, such as cachexia, osteoporosis, neuropathic pain, depression, hypertension, malnutrition-related obesity, and associated inflammatory diseases.

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.

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.

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.

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.

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

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

HS014 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 modulates the behavioral effects of morphine in mice. HS014 increases food intake in free-feeding rats.

Agouti-related Protein (AGRP) (83-132) Amide (human) is a fragment of agouti-related protein (AGRP) which is a protein found in abundance in the arcuate nucleus of the hypothalamus. AgRP primarily acts as an inverse agonist for the melanocortin-4 receptor (MC4R) to increase food intake.

JKC363 TFA, 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). JKC363 TFA blocks the stimulatory effect of α-MSH on TRH release. Anti-hyperalgesic effect.

MC4R Antagonist-1 (compound 1) is an MC4R-selective antagonist (IC₅₀<10 nM). MC4R Antagonist-1 can be used for the research of cachexia, anorexia, anorexia nervosa, involuntary weight loss, failure to thrive, sarcopenia, muscle wasting, muscle weakness, frailty, osteoporosis.