melanocortin-1 receptor

Dersimelagon (MT-7117) 是一种具有口服活性的选择性黑皮质素 1 受体(MC1R) 激动剂，对人 (h)、食蟹猴 (cm)、小鼠 (m) 和大鼠 (r) MC1R 的 EC50 值分别为 8.16、3.91、1.14 和 0.251 nM。Dersimelagon 对 hMC1R 和 hMC4R 表现出良好的亲和力，Ki 值分别为 2.26 和 32.9 nM。Dersimelagon 可用于皮肤色素沉着的研究[1]。

AP1189 acetate 是黑皮质素 1 和黑皮质素 3 受体的偏向激动剂。

JNJ-10229570 (UNII-N9IX402L35) 是肾上腺皮质受体 1 和肾上腺皮质受体 5 的拮抗剂，可抑制皮脂腺分化和皮质特异性脂质的产生，其抑制125I-NDP-α-MSH 和人类细胞中 MC1R 和 MC5R 结合的IC50值分别为 270 nM 和 200 nM。

Afamelanotide acetate 是一种合成的 α-黑素细胞刺激激素类似物和一流的黑皮质素-1 受体激动剂，用于治疗红细胞生成性原卟啉症。

BMS-470539 dihydrochloride 是一种具有选择性和高效性的黑皮质素 1 受体 (MC-1 R) 激动剂，具有抗炎活性。 BMS-470539 在新生儿缺氧缺血大鼠模型中通过 MC1R cAMP PKA Nurr1 信号通路减轻氧化应激和神经元凋亡。

ACTH (1-17) acetate 是一种有效的人黑皮质素 1 (MC1) 受体激动剂，具有高亲和力 (Ki = 0.21 nM)。

α-MSH (MSH, amide) 是一种内源性神经肽，是一种内源性黑皮质素受体 4 (MC4R) 激动剂，具有抗炎和解热活性。

MCL0020 是一种有效的选择性黑素皮质素MC4受体拮抗剂，IC50为 11.63 nM。它剂量依赖性减轻束缚应激诱发的厌食症，在体内表现出抗焦虑样活性。

Nonapeptide-1 acetate salt (158563-45-2 free base) (Melanostatine-5 acetate salt) 是一种肽激素，是一种有效的 α-黑色素细胞刺激素 (α-MSH) 拮抗剂，IC50 为 11 nM。

β-Melanocyte Stimulating Hormone (MSH), human (Synonyms: Beta-MSH (1-22) (human)) β-Melanocyte Stimulating Hormone (MSH), human, a 22-residue peptide, acts as an endogenous melanocortin-4 receptor (MC4-R) agonist.

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)

Adrenocorticotropic Hormone (ACTH) (1-39), rat, is a potent melanocortin 2 (MC2) receptor agonist. During in vitro incubation with membrane preparations, peptide fragments of ACTH (1-39) were formed and subsequently isolated by high-pressure methods.

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

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。

TCMCB07 TFA为一环状九肽，属口服活性及脑渗透性黑皮质素受体4 (MC4R) 拮抗剂，于恶病质中扮演关键角色。

'(p-Iodo-Phe7)-ACTH (4-10)'为垂体前腺产生和分泌的肾上腺皮质激素(ACTH)衍生物，担任黑素皮质素(MC)受体拮抗剂角色，能够抑制α-黑素细胞刺激激素(α-MSH)引发的大鼠过度梳理行为。

Nonapeptide-1 (Melanostatine™ 5) 可以抑制黑色素的合成，这使得它对治疗某些皮肤病很感兴趣。

ACTH (1-17) TFA is a corticotrophin analogue and an effective human melanocortin 1 (MC1) receptor agonist with Ki value of 0.21 nM.

Adrenocorticotropic Hormone (ACTH) (1-39), rat (TFA) is a potent melanocortin 2 receptor (MC2) agonist.

Beta-MSH (1-22) (human) acetate (Beta-MSH (1-22) (human) acetate (17908-57-5 Free base)) 是一种 22 肽，是一种内源性黑皮质素 4 受体 (MC4-R) 激动剂。

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.

γ-1-Melanocyte Stimulating Hormone (MSH), amide为含11个氨基酸的多肽，主要通过激活黑皮质素受体3 (MC3-R) 调节钠 (Na+) 平衡及血压。

PG106 TFA 是一种有效的、选择性的 hMC3 receptor 拮抗剂 (IC50= 210 nM)，对 hMC4 受体(EC50=9900 nM) 和 hMC5 受体无活性。

CCZ01048 TFA 是一种 α-MSH 类似物，与黑素皮质素1受体(MC1R)具有很高的结合亲和力，Ki 值为 0.31 nM。CCZ01048 TFA 具有快速内化 B16F10 黑色素瘤细胞和高体内稳定性。CCZ01048 TFA 是恶性黑色素瘤 PET 显像的一个有前途的制剂。