MC1R Agonist

Setmelanotide (RM-493) is a blood-brain barrier-permeable, selective MC4R agonist with a K_i value of 2.1 nM for hMC4R. Setmelanotide activates the CaMKK2/AMPK signaling pathway. Setmelanotide 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 is applicable to research related to obesity, hyperinsulinemia, fatty liver and respiratory depression.

Melanotan 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.

BMS-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.

Resomelagon (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.

ACTH (1-17) TFA, an adrenocorticotropin analogue, is a potent human melanocortin 1 (MC1) receptor agonist with a K_i of 0.21 nM.

Setmelanotide monoacetate (RM-493 monoacetate) is a blood-brain barrier-permeable, selective MC4R agonist with a K_i 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 (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.

Setmelanotide TFA (RM-493 TFA) is a blood-brain barrier-permeable, selective MC4R agonist with a K_i value of 2.1 nM for hMC4R. Setmelanotide TFA activates the CaMKK2/AMPK signaling pathway. Setmelanotide TFA 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 TFA is applicable to research related to obesity, hyperinsulinemia, fatty liver and respiratory depression.

RY746 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.

(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 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.