Melanocortin Receptor Agonist

Filimelnotide is a agonist of melanocortin receptor.

PF-00446687 hydrochloride is a potent, brain-penetrating, selective melanocortin 4 receptor (MC4R) agonist with an EC₅₀ of 12 nM. PF-00446687 hydrochloride can be used in the research of 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.

Filimelnotide acetate is a melanocortin receptor agonist.

BMS-470539 is a synthetic MC-1R agonist with potent anti-inflammatory properties. BMS-470539 selectively activates human and murine MC-1R with EC50 values ??of 16.8 nM and 11.6 nM, respectively. In vitro studies have shown that BMS-470539 is able to dose-dependently inhibit TNF-alpha-induced NF-kB activation in human melanoma cells expressing MC-1R. In vivo, subcutaneous injection of BMS-470539 into BALB/c mice effectively inhibited LPS-induced TNF-alpha production with an ED50 of approximately 10 μmol/kg and a pharmacodynamic half-life of approximately 8 hours. It also significantly reduced leukocyte infiltration in a lung inflammation model and attenuated paw swelling in a delayed-type hypersensitivity model, highlighting its efficacy as an anti-inflammatory agent through MC-1R modulation.

[D-Trp8]-γ-MSH TFA is a potent and selective agonist of melanocortin 3 (MC3) receptor, with IC₅₀s of 6.7 nM, 600 nM and 340 nM for hMC3, hMC4 and hMC5, respectively in CHO cells. [D-Trp8]-γ-MSH TFA could provide protection against multiple inflammatory disorders such as rheumatoid arthritis and colitis.

Bivamelagon-d₈ (MC-4R Agonist 2-d₈) is the deuterium labeled Bivamelagon (HY-153660). Bivamelagon (MC-4R Agonist 2) is an orally active MC4R agonist with EC₅₀ values of 0.562 nM (Luci assay) and 36.5 nM (cAMP assay), and a K_i of 65 nM. Bivamelagon can be used for the research of diseases such as obesity and diabetes.

Alsactide, a heptadecapeptide analogue, is an adrenocorticotropic hormone (ACTH) agonist. Alsactide can be used in research of central nervous system.

α-MSH free acid (α-Melanocyte-Stimulating Hormone free acid) is an MC3R and MC4R agonist with EC₅₀s of 0.16 nM and 5.6 nM, respectively. α-MSH free acid activates cAMP generation at MC3R and MC4R.

Fenoprofen-¹³C₆ (LILLY-53858-¹³C₆) sodium hydrate is the ¹³C labeled Fenoprofen (HY-B1456A).Fenoprofen (LILLY-53858) is a nonsteroidal anti-inflammatory agent (NSAID) and inhibits cyclooxygenase (COX). Fenoprofen is a melanocortin receptors (MCRs) positive allosteric modulator (PAM). Fenoprofen also increases ERK1/2 activation in HEK293T cells. Fenoprofen has anti-arthritic activities and can be used for the study of rheumatoid arthritis and osteoarthritis.

CTX-1211 is a selective, orally effective melanocortin MC4R agonist (EC₅₀=0.38 nM). CTX-1211 can enhance the feeding suppression and weight loss effects induced by liraglutide (HY-P0014), and promote anorexia and weight loss activity. CTX-1211 is mainly used in the study of obesity and other metabolic disorders.

RO27-3225 is potent and selective melanocortin 4 receptor (MC4R) agonist with an EC₅₀ of 1 nM and 8 nM for MC4R and MC1R, respectively. RO27-3225 shows 30-fold selectivity for MC4R over MC3R. RO27-3225 has neuroprotective and anti-inflammatory effects.

Lys-γ3-MSH(human) is a melanocortin peptide derived from the C-terminal of the fragment of pro-opiomelanocortin (POMC). Lys-γ3-MSH(human) potentiates the steroidogenic response of the rat adrenal to adrenocorticotrophin (ACTH). Lys-γ3-MSH(human) is a potent stimulator of lipolysis with an apparent EC₅₀ of 3.56 nM. Lys-γ3-MSH(human) can activate hormone sensitive lipase (HSL) and Perilipin A resulting in lipolysis.

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

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.

PG-931 TFA, an analog of SHU 9119 (HY-P0227), is a potent melanocortin 4 (MC4) receptor (IC₅₀=0.58 nM) agonist and is more selective than for the hMC3R (IC₅₀=55 nM) or the hMC5R(IC₅₀=2.4 nM). PG-931 TFA can reverse haemorrhagic shock and prevent multiple organ damage in vivo.

Melanotan (MT)-II acetate is a melanocortin receptor agonist. Melanotan (MT)-II acetate activates melanocortin receptor 3 and melanocortin receptor 4, and stimulates the release of central endogenous oxytocin. Melanotan (MT)-II acetate reverses recognition memory impairment, increased anxiety levels and reduced exploratory tendency in zebrafish exposed to short-term high-fat diet. Melanotan (MT)-II acetate improves impaired social behavior indicators in mouse models of autism spectrum disorder. Melanotan (MT)-II acetate induces weight loss, reduces food intake and exerts anorectic effects. Melanotan (MT)-II acetate increases intracavernous pressure and erectile activity in brown rats. Melanotan (MT)-II acetate can be used in studies related to memory impairment, anxiety, reduced exploratory behavior, autism spectrum disorder, obesity and erectile dysfunction.

MK-0489 is an orally active, highly effective, and selective MC4R agonist. MK-0489 exhibits a strong binding affinity (IC₅₀ = 13 nM) and functional agonist activity (EC₅₀ = 4.6 nM) at human MC4R. MK-0489 shows functional activity of 22 nM (EC₅₀) on mouse MC4R and 1.7 μM (EC₅₀) on mouse MC3R. MK-0489 can be used for the study of obesity.

γ1-MSH TFA is a melanocortin MC3 receptor agonist, with a K_i of 34 nM for the rat MC3 receptor. γ1-MSH TFA displays ~40-fold selectivity over MC4 (K_i=1318 nM).

Bivamelagon (MC-4R Agonist 2) hydrochloride is an orally active and BBB-penetrable MC4R agonist with EC₅₀ values of 0.562 nM (Luci assay) and 36.5 nM (cAMP assay), and a K_i of 65 nM. Bivamelagon hydrochloride can be used for the research of diseases such as obesity and diabetes.