human plasma

Copper tripeptide (GHK-Cu) 是天然存在的三肽，首先从人血浆中分离，但也能够在唾液和尿液中发现。它能够提高成纤维细胞中胶原蛋白，弹性蛋白，蛋白多糖和糖胺聚糖中信使 RNA 的产生。在伤口愈合期间，它能够通过蛋白水解从现有的细胞外蛋白质中除去，并且用作炎性和内皮细胞的化学引诱物。它是皮肤再生中多种细胞途径的天然调节剂。

Alpha 1 Antichymotrypsin, Human Plasma 是一种丝氨酸蛋白酶 (serine protease) 抑制剂，出现在阿尔茨海默症的淀粉样病变中，可用于阿尔茨海默症研究。

Somatostatin 1-28 acetate 在人源血浆中循环。 血浆中约 46% 的总生长抑素样免疫反应性是由于 Somatostatin 1-28 acetate 所致。

Human serum albumin（人血清白蛋白，HSA）是人类血浆中含量最多的蛋白质，在肝脏中产生并且可溶于水，分子量为66.5 kDa。HSA通过选择性结合交叉结构的 A 寡聚体，抑制阿尔茨海默病。HSA是淀粉样蛋白-β （Αβ）聚集的关键内源性抑制剂。HSA在细胞培养中作为载体蛋白，用于运输脂肪酸、类固醇和甲状腺激素，并调节血液的渗透压；还用于药物递送研究、免疫分析和细胞冻存。

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)

Osteocalcin (1-49) is a non-collagenous peptide that is secreted by osteoblasts and odontoblasts and comprises 1-2% of the total protein in bone. Secretion of osteocalcin (1-49) is stimulated by 1,25-dihydroxy vitamin D and plasma levels increase in diseases that induce dysregulated bone turnover such as osteoporosis, Paget's disease, and primary hyperparathyroidism. Osteocalcin (1-49) is positively correlated with insulin sensitivity and negatively correlated with high blood glucose levels in women. In vitro, osteocalcin induces chemotaxis of MDA-MB-231 breast cancer cells, human peripheral blood monocytes, and rat osteosarcoma cells with osteoblast-like characteristics. It is also expressed by vascular smooth muscle cells (VSMCs) displaying an osteoblast-like phenotype and has been positively associated with calcification of aortic tissue and heart valves in humans.

Obestatin is a 23 amino acid peptide hormone with a conserved C-terminal glycine residue and amidation site that is formed by cleavage of the ghrelin and obestatin prepropeptide.1It binds to the orphan receptor GPR39 (Kd= 1 nM) and stimulates cAMP production in CHO and HEK293 cells overexpressing human GPR39. Obestatin inhibits contraction of isolated mouse jejunum muscle strips induced by ghrelin .In vivo, obestatin (12.5-1,000 nmol/kg) suppresses food intake in a time- and dose-dependent manner and reduces body weight gain and gastric emptying in mice. Obestatin (0.22 g per animal) also reduces food intake and glucose response without affecting plasma insulin responses in fasted high-fat diet fed mice.2 1.Zhang, J.V., Ren, P.C., Avsian-Kretchmer, O., et al.Obestatin, a peptide encoded by the ghrelin gene, opposes ghrelin's effects on food intakeScience310(5750)996-999(2005) 2.Subasinghage, A.P., Green, B.D., Flatt, P.R., et al.Metabolic and structural properties of human obestatin {1-23} and two fragment peptidesPeptides31(9)1697-1705(2010)

Pituitary adenylate cyclase-activating peptide (PACAP) (6-27) is a PACAP receptor antagonist with IC50 values of 1,500, 600, and 300 nM, respectively, for rat PAC1, rat VPAC1, and human VPAC2 recombinant receptors expressed in CHO cells. It binds to PACAP receptors on SH-SY5Y and SK-N-MC human neuroblastoma and T47D human breast cancer cells (IC50s = 24.5, 106, and 105 nM, respectively) and inhibits cAMP accumulation induced by PACAP (1-38) (Kis = 457, 102, and 283 nM, respectively, in SH-SY5Y, SK-N-MC, and T47D cells). In vivo, in newborn pigs, PACAP (6-27) (10 μM) inhibits vasodilation of pial arterioles induced by PACAP (1-27) and PACAP (1-38) . It also inhibits PACAP (1-27)-stimulated increases in plasma insulin and glucagon levels and pancreatic venous blood flow in dogs when administered locally to the pancreas at a dose of 500 μg.

Neuropeptide SF (human) acetate 是一种神经肽，可增强心室旁 CRH 的释放并增加血浆中的 ACTH 和皮质酮水平。

RFRP-1(human) TFA, an endogenous NPFF receptor agonist, exhibits potent activity with EC50 values of 0.0011 nM for NPFF2 and 29 nM for NPFF1. It significantly diminishes the contractile function of isolated rat and rabbit cardiac myocytes. Moreover, it decreases heart rate, stroke volume, ejection fraction, and cardiac output, while elevating plasma prolactin levels in rats.

TAK-683 acetate是一种高效的KISS1R激动剂(IC50=170 pM)，改善了代谢稳定性。作为九肽metastin的类似物，对人和大鼠的EC50值分别为0.96 nM和1.6 nM。该化合物通过消耗下丘脑GnRH，能够降低血浆FSH、LH、睾酮水平，展示了对研究激素依赖性前列腺癌的潜力。

pTH-Related Protein (1-40) (human, mouse, rat) 促进大鼠肠细胞通过PTHR1受体和PKCα/β信号通路的钙吸收作用。该蛋白增加了甲状旁腺激素1受体（PTHR1）表达，提升了四种跨膜钙转运蛋白—TRPV6、CaBP-D9k、NCX1和PMCA1的水平。

Bz-Ala-Arg为特定的二肽，既是人胰腺羧肽酶B又是血浆羧肽酶N的分光光度底物（0.4 M 吡啶甲酸，pH 4.25）。此外，Bz-Ala-Arg亦可用于筛选上述两种酶的竞争性抑制剂。

GRPP (human)为含有30个氨基酸的Gcg衍生肽。该化合物能引起血浆胰岛素的轻微上升及血浆胰高血糖素的轻微降低，但不会影响大鼠胰岛内的胰岛素分泌。

Pegylated synthetic human c-peptide 保留与天然（即非聚乙二醇化）C 肽相当的生物活性，且延长了在血浆中的循环停留时间，适用于糖尿病性周围神经病变的研究。

胃抑制肽(GIP) (22-51) 是一种具有30个氨基酸的前动脉硬化肽，对应于GIP前体蛋白proGIP的第22至51个氨基酸残基，已在人类血浆中发现。在1 µM的浓度下使用，该肽能引起在巨峰细胞分化的THP-1细胞和分离的人类主动脉内皮细胞中IκB-α的降解和NF-κB的核转移。在体内，GIP (22-51) 增加了ApoE-/-小鼠的动脉粥样硬化病变面积和斑块形成。

Cys-pexiganan是一种抗微生物肽，是pexiganan的衍生物，具有N-末端的半胱氨酸。它对P. aeruginosa和S. aureus具有活性（MICs分别为64和16 µg/ml）。Cys-pexiganan与含醋酸纤维素的聚乙烯醇电纺垫结合，可以加速隔离的重钙化人类血浆的凝血。

1-Linoleoyl LPA（1-亚油酰LPA）是LPA2受体的激动剂，属于一种含有亚油酸的甘油磷脂，在sn-1位置含亚油酸。它是小鼠和人体血浆中最丰富的LPA。1-Linoleoyl LPA在表达LPA2受体的Sf9细胞中选择性地增加细胞内钙水平（EC50约为10 nM），相较于表达LPA1和LPA3受体的Sf9细胞（EC50分别约为200和80 nM）。携带NCTC克隆2472肿瘤的小鼠中，1-linoleoyl LPA的血清水平增加。与患有初发进行性多发性硬化症的患者相比，复发缓解型多发性硬化症患者的血浆1-Linoleoyl LPA水平降低，且与神经功能缺损严重程度负相关。

Tirzepatide 是一种glucagon-like peptide 1 receptor (GLP-1R) 和 G protein-coupled receptor 119 (GPR119)的激动剂。它在表达人类GLP-1R或GPR119的HEK293细胞中诱导cAMP的产生（EC50s分别为6.54和1.01 nM）。Tirzepatide（100 nM）在表达人类GLP-1R或GPR119的HEK293细胞中诱导受体内化。在体内，Tirzepatide（每天10 nmol/kg）降低高脂饮食诱导的肥胖小鼠模型的体重、食物摄入量、血浆leptin、三酸甘油酯和free fatty acids (FFAs)水平、肝脏三酸甘油酯和血糖水平。它通过每三天给药50 nmol/kg的剂量，阻止A. alternata诱导的A. alternata挑战小鼠的支气管肺泡灌洗液（BALF）中嗜酸性粒细胞和淋巴细胞数量的增加。Tirzepatide（每三天50 nmol/kg）抑制由毒蕈碱受体激动剂methacholine (acetyl-β-methylcholine)导致的在糖尿病诱导的哮喘小鼠模型中的支气管收缩。含Tirzepatide的制剂已用于治疗2型糖尿病。

Kinetensin acetate(103131-69-7 free base) 是从经胃蛋白酶处理的人血浆中分离出来的。它是一种神经降压素样肽。

RFRP-1 (human) acetate(311309-25-8 free base) 是一种有效的内源性 NPFF 受体激动剂（NPFF2 和 NPFF1 的 EC50 值分别为 0.0011 和 29 nM）。它减弱离体大鼠和兔心肌细胞的收缩功能。降低心率、每搏输出量、射血分数和心输出量，并增加大鼠的血浆催乳素水平。 GnIH 同系物。

KSL 128114是一种syntenin肽抑制剂，能结合syntenin的PDZ1结构域，其亲和力达到纳摩尔级。在人血浆和鼠肝微粒体中，KSL 128114不易被降解，并且对syntenin具有PDZ结构域的选择性。

Caloxin 1b3 是一种肽，作为选择性血浆膜钙离子泵 1 (PMCA1) 抑制剂，对兔十二指肠粘膜中PMCA1的Ca2+–Mg2+-ATPase抑制作用比对人红细胞中PMCA4的更强。此外，Caloxin 1b3 能增加内皮细胞胞浆中的Ca2+浓度，它可用于心血管疾病研究。