a-msh tfa

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)

Lys-γ3-MSH(human) TFA是源自POMC片段C端的黑素皮质素肽，具备增强大鼠肾上腺对促肾上腺皮质激素(ACTH)的类固醇生成反应的能力。该化合物作为一种有效的脂解激活剂，其表观EC50值为3.56 nM，能够激活激素敏感脂肪酶(HSL)和紫苏脂素A，进而促进脂解。

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。

[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。

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。

beta-MSH, human 是一种由促黑素皮质素（POMC）产生的内源性多肽激素和神经递质，是MC4-R(melanocortin 4 receptor)的激动剂。

Melanostatin, frog TFA 是一种高效性的 α-黑素细胞刺激激素 (α-MSH) 释放抑制剂，是从青蛙大脑中分离出的一种 36 个氨基酸的肽，通过调节 K+、Na+ 和 Ca2+ 电流抑制青蛙黑素营养素的电活性。