Melanocortin Receptor

Amphistin是一种黑素生成 (melanogenesis) 抑制剂，存在于放线菌中。Amphistin抑制B16黑色素瘤细胞的黑素生成，但不干扰细胞生长。

Delmadinone acetate 是一种能够在口服后调节雌性和雄性宠物发情及排卵的化合物。它通过抑制垂体释放 ACTH 导致肾上腺受到抑制。

(2R,2R)-PF-07258669 是MC4R(黑色素皮质素 4 受体)的一种拮抗剂，主要应用于食欲与能量消耗调节的研究领域。

MCL0129, a selective and non-peptidergic melanocortin 4 (MC4) receptor antagonist, is a potential treatment for cachexia.

Ebiratide is an analog of ACTH 4-9.

Filimelnotide 是一种激活黑皮质素受体的激动剂。

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。

a-MSH, amide Acetate(581-05-5 free base) 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。 α-MSH 是阿片黑皮质素原 (POMC) 的翻译后衍生物。

ACTH 11-24 acetate(4237-93-8 free base) (Adrenocorticotropic Hormone (11-24) acetate) 是促肾上腺皮质激素的片段，可诱导皮质醇释放。 ACTH (11-24) 已被确定为分离的肾上腺细胞中 ACTH (1-39) 和 ACTH (1-10) 的竞争性拮抗剂。

HS 014 acetate(207678-81-7 free base) 是一种有效的选择性黑皮质素 MC4 受体拮抗剂（克隆的人 MC4、MC1、MC3 和 MC5 受体的 Ki 值分别为 3.16、108、54.4 和 694 nM）。体内中枢给药后增加大鼠的食物摄入和小鼠的伤害感受。还抑制室旁下丘脑中 IL-1β 诱导的 Fos 表达。

Endogenous melanocortin MC3 receptor agonist (pKi = 7.46) that displays ~ 40-fold selectivity over MC4. Increases the release of extracellular dopamine, which induces grooming and vertical activity (rearing) in rats. Exhibits hypertensive, tachycardic and

Melanocortin (MC) 3-MSH (Melanocyte-Stimulating Hormone) is believed to signal through the MC 3 receptor. It induces a sustained increase in intracellular free calcium levels ([Ca2+]i) in a subpopulation of pituitary cells. Most of the cells responding to

Setmelanotide（RM-493）是一种选择性的黑皮质素-4 受体激动剂，对人源和大鼠 MC4R 的 EC50 分别为 0.27 和 0.28 nM。Setmelanotide 可增强 cAMP 信号传导，并通过激活交感神经节前神经元影响血压调控，广泛用于研究 MC4R–MRAP2 相互作用。Setmelanotide 可通过调节饥饿与饱腹通路，因此也应用于肥胖相关研究。研究表明，Setmelanotide 可逆转小鼠中利培酮诱导的体重增加。此外，Setmelanotide 在星形胶质瘤细胞中的抗炎作用及其与热量限制联合应用的研究进一步体现了其在代谢与神经内分泌研究中的广泛价值。

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

Adrenocorticotropic Hormone (ACTH) (4-10), human是黑皮质素 4 型受体 (melanocortin 4 receptor, MC4R) 激动剂。

γ3-MSH 源于 pro-opiomelanocortin (POMC) 的 N 端，能够激活人肾上腺肿瘤细胞分泌醛固酮。

Potent and selective melanocortin 4 (MC4) receptor agonist (IC50 values are 0.58 and 55 nM for human MC4 and MC3 receptors respectively). Produces a rapid and dose dependent restoration of cardiovascular and respiratory function in hemorrhage-shocked rats

'(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。

Tetrapeptide-1，一种生物活性肽，具抗氧化功能，已报道应用于化妆品成分。

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。

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)

Potent and selective melanocortin MC4 receptor antagonist (Ki values are 3.16, 108, 54.4 and 694 nM for cloned human MC4, MC1, MC3 and MC5 receptors respectively). Increases food intake in rats and nociception in mice following central administration in v

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。

ACTH (22-39) is a fragment of the adrenocorticotropic hormone (ACTH), specifically comprising the 22-39 sequence of ACTH.

Setmelanotide Acetate(920014-72-8 free base) (RM-493 Acetate) 是黑皮质素 4 受体 (MC4R) 的选择性激动剂（人和大鼠 MC4R，EC50 分别为 0.27 nM 和 0.28 nM）。

Isodocarpin 是一种天然产物，可用于生命科学领域的相关研究。其产品编号为 TN5604，CAS号为 10391-08-9。

Ganodermanondiol是一种天然的黑色素(Melanogenesis)抑制剂，能够在B16F10细胞中抑制tyrosinase，TRP-1，TRP-2和MITF，影响MAPK和cAMP。Ganodermanondiol还具有抗炎作用和护肝作用，影响Nrf2依赖的HO-1和AMPK。

Bremelanotide is a synthetic peptide analog of alpha-MSH and is an agonist at melanocortin receptors including the MC3R and MC4R.

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。

Chlorophorin shows high anti-protozoal activity with an MIC of 0.25 microg/ml. Chlorophorin can strongly inhibit mushroom tyrosinase activity with IC50 values of 2.5 ± 0.408 uM; it inhibits α-melanocyte-stimulating hormone-induced melanin production in B16F10 melanoma cells.