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]。

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。

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。

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

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。

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.

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

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)

Resomelagon (AP1189) 是具有口服活性的有效黑素皮质素受体 (MR) 激动剂，可诱导Ca2+流动和 ERK1 2 磷酸化。Resomelagon 显示出抗炎活性， 可用于研究肥胖和慢性炎症。

Dersimelagon phosphate is a selective melanocortin-1 receptor (MC1R) agonist that increases skin melanin without sun exposure and is being developed to increase light tolerance in EPP XLP patients.

RO27-3225, also known as RO273225 is a melanocortin type 4 receptor agonist with EC50 = 1 nM. It may alleviate intestinal dysfuntion and brain damage. It has been investigated for an anti-obesity medication. Ro 27-3225 shows some activity at the MC1 receptor. Ro 27-3225 reverses hemorrhagic shock, reduces multiple organ damage, and improves survival.

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.

Nonapeptide-1 (Melanostatine-5) acetate salt，一种多肽类激素，是 MC1R 选择性拮抗剂 (Ki: 40 nM)。 Nonapeptide-1 acetate salt 是一种竞争性的α-MSH 拮抗剂，可有效抑制黑素细胞中 α-MSH 诱导的细胞内 cAMP 和黑素体扩散 (IC50分别为 2.5 nM 和 11 nM)。 Nonapeptide-1 acetate salt 抑制黑色素合成，可用于研究皮肤色素沉着和肾上腺类固醇生成的调节、皮肤癌。

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。

JKC363 TFA为选择性MC4受体拮抗剂，MC4受体(IC50=0.5 nM)亲和力是MC3受体(44.9 nM)的90倍。JKC363 TFA能阻断α-MSH对TRH释放的刺激，显示出抗痛觉效果。

γ1-MSH TFA 是黑素皮质素 MC3受体激动剂，对大鼠 MC3受体的 Ki 为 34 nM。γ1-MSH TFA 在 MC4 (Ki=1318 nM) 上表现出约 40 倍的选择性。

HS014 TFA 是一种高效、选择性的黑素皮质素-4(MC4)受体拮抗剂，对人 MC4、MC1、MC3 和 MC5 受体的Ki 值分别为 3.16、108、54.4 和 694 nM。HS014 TFA 增加自由喂养大鼠的食物摄取量。

[D-Trp8]-γ-MSH TFA 是一种有效的、选择性的黑皮质素3 (MC3)受体激动剂，在 CHO 细胞中，抑制 hMC3，hMC4和 hMC5的 IC50值分别为 6.7 nM，600 nM 和 340 nM。[D-Trp8]-γ-MSH TFA 显示出对多种炎症性疾病(如类风湿关节炎和结肠炎)的保护作用。

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。

ACTH (1-17) TFA 是促肾上腺皮质激素类似物，是一种有效的人黑皮素受体 (human melanocortin 1 (MC1) receptor) 激动剂，Ki 值为 0.21 nM。

CCZ01048 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 具有快速内化 B16F10 黑色素瘤细胞和高体内稳定性。CCZ01048 是恶性黑色素瘤 PET 显像的一个有前途的制剂。