mc4r agonist 1

MC-4R Agonist 1 is an agonist of human melanocortin-4 receptor (MC-4R) and can be used in the research of sexual dysfunction, obesity, and diabetes.

PF-00446687 is a selective agonist of melanocortin-4 receptor (MC4R) (EC50 of 12 ± 1 nM).

α-Melanocyte-stimulating hormone (α-MSH) is a 13-amino acid peptide hormone produced by post-translational processing of proopiomelanocortin (POMC) in the pituitary gland, as well as in keratinocytes, astrocytes, monocytes, and gastrointestinal cells.1It is an agonist of melanocortin receptor 3 (MC3R) and MC4R that induces cAMP production in Hepa cells expressing the human receptors (EC50s = 0.16 and 56 nM, respectively).2α-MSH (100 pM) reducesS. aureuscolony formation andC. albicansgerm tube formationin vitro.3It inhibits endotoxin-, ceramide-, TNF-α-, or okadaic acid-induced activation of NF-κB in U937 cells.1α-MSH reduces IL-6- or TNF-α-induced ear edema in mice.4It also prevents the development of adjuvant-induced arthritis in rats and increases survival in a mouse model of septic shock. Increased plasma levels of α-MSH are positively correlated with delayed disease progression and reduced death in patients with HIV.1 1.Catania, A., Airaghi, L., Colombo, G., et al.α-melanocyte-stimulating hormone in normal human physiology and disease statesTrends Endocrinol. Metab.11(8)304-308(2000) 2.Miwa, H., Gantz, I., Konda, Y., et al.Structural determinants of the melanocortin peptides required for activation of melanocortin-3 and melanocortin-4 receptorsJ. Pharmacol. Exp. Ther.273(1)367-372(1995) 3.Cutuli, M., Cristiani, S., Lipton, J.M., et al.Antimicrobial effects of a-MSH peptidesJ. Leukoc. Biol.67(2)233-239(2000) 4.Lipton, J.M., Ceriani, G., Macaluso, A., et al.Antiiinflammatory effect of the neuropeptide a-MSH in acute, chronic, and systemic inflammationAnn. N.Y. Acad. Sci.25(741)137-148(1994)

Melanotan II acetate is an agonist of melanocortin receptor 1 (MC1R), MC3R, MC4R, and MC5R. It has been shown to improve recovery of sciatic nerve function after mechanical injury and increase cisplatin-induced decreases in sensory nerve conduction velocity. Melanotan II acetate increases oxygen consumption and protein levels of uncoupling protein 1 (UCP1) in brown adipose tissue homogenates and decreases food intake, body weight, and serum levels of leptin, glucose, insulin, and cholesterol.

Agouti-related Protein (AGRP) (83-132) Amide (human)，一种AGRP的片段，主要在下丘脑弓状核中表达。该化合物主要通过作为黑皮质素-4受体(MC4R)的反向激动剂来增加食物摄入。

MC-4R Agonist 2 (实施例 1)作为MC4R激动剂，适用于肥胖、糖尿病、炎症及勃起功能障碍的研究领域。

MC-4R Agonist 2 hydrochloride (实施例 1) 是用于研究肥胖、糖尿病、炎症和勃起功能障碍的MC4R激动剂。

Ac-DArg-c[Cys-Glu-His-DPhe-Arg-Trp-Cys]-NH2 是一种环状八肽，能够激活MC4R。该化合物能显著提高心率与血压。

RO27-3225 TFA is a potent and selective agonist of melanocortin 4 receptor (MC4R; EC50: 1 nM and 8 nM for MC4R and MC1R) with neuroprotective and anti-inflammatory effects. RO27-3225 TFA shows ~30-fold selectivity for MC4R over MC3R.