GLP-1/GCG 蛋白, Human (HEK293, His)

GLP-1 and GCG are two proteins derived from the same precursor protein, which is encoded by the GCG-glucagon gene. The GCG protein is a counterregulatory hormone to insulin, playing a crucial role in glucose metabolism by increasing gluconeogenesis and reducing glycolysis to regulate blood glucose levels. GLP-1 protein, secreted by intestinal endocrine cells, promotes insulin secretion, regulates gastrointestinal motility, and inhibits the secretion of GCG protein. GLP-1/GCG protein, Human (HEK293, His), is a recombinant GLP-1/GCG protein expressed by HEK293 cells, with a His tag at the C-terminus, and is composed of 160 amino acids (R21-K180)^{[1][2][3][4][5][6][7][8][9][10]}.

GCG 蛋白，又称为胰高血糖素 (Glucagon)，由胰腺 α 细胞分泌，在葡萄糖代谢和稳态维持发挥重要作用。作为胰岛素的反调节激素，GCG 蛋白在体内血糖水平下降时，能够对抗胰岛素的降糖作用，通过增加血糖水平来维持体内的血糖平衡。在糖尿病中，GCG 蛋白在启动和维持高血糖状态方面发挥重要作用。除调节葡萄糖代谢之外，GCG 蛋白也参与脂质代谢调节^[1][2][3]。
GLP-1 蛋白是一种由肠道分泌的激素，在调节血糖水平和维护胃肠功能功能方面具有重要作用。
血糖调节：GLP-1 蛋白通过与胰岛β细胞表面受体结合，来增强胰腺 β 细胞对葡萄糖的感应，使其在血糖水平较高时分泌更多的胰岛素。同时 GLP-1蛋白可以促进胰岛细胞新生和胰腺 β 细胞增殖，并可能抑制 β 细胞的凋亡，从而保护胰岛功能^[4]。
胃肠功能：GLP-1 蛋白可通过抑制 GCG 蛋白分泌来维护正常的胃肠功能，还可通过调节饱腹感来增强外周组织对葡萄糖的摄取、利用和储存。同时 GLP-1 蛋白对肠道上皮生长具有促进作用，有助于维持肠道健康^[5]。
此外，GLP-1蛋白可以通过影响 LH、TSH、CRH、催产素和抗利尿激素的分泌来调节下丘脑-垂体轴 (HPA) ^[5]。
GLP-1 蛋白通过减少炎症细胞因子的产生和免疫细胞在组织中的浸润，对胰岛和脂肪组织具有抗炎作用，此外在一些慢性炎症疾中，包括 1 型和 2 型糖尿病、动脉粥样硬化、神经退行性疾病、非酒精性脂肪性肝炎、糖尿病肾病等，GLP-1 蛋白也显示出抗炎作用^[6]。

GCG 蛋白 (Human) (100 nM，1 小时) 在生理浓度的葡萄糖 (5 mM) 刺激下可通过结合胰腺 β 细胞上的 GCG 蛋白受体来增强胰岛素分泌^[7]。
在将胰腺 α 细胞长期暴露于 GLP-1 蛋白 (Human) (100 nM，72 小时) 的条件下，GLP-1 蛋白 (Human) 会通过刺激转录因子 Pax6 和蛋白转化酶 PC1/3 来促进胰腺 α 细胞合成和释放 GLP-1^[8]。

GCG 蛋白 (Human) (150 μg/kg，腹腔注射，每日一次，共 5 天) 可以在 Sprague-Dawley 大鼠体内刺激棕色脂肪细胞产热^[9]。
GCG蛋白 (Human) (0.3 μg/kg 和 0.6 μg/kg，腹腔注射，单次给药；0.6 μg/kg，皮下注射，单次给药) 会引起雌性农场猪体内葡萄糖水平显著升高，且相比于皮下注射，通过腹腔注射给药会引起更快速的血糖上升响应^[10]。

Human

HEK293

C-6*His

P01275 (R21-K180)

2641  [NCBI]

RSLQDTEEKSRSFSASQADPLSDPDQMNEDKRHSQGTFTSDYSKYLDSRRAQDFVQWLMNTKRNRNNIAKRHDEFERHAEGTFTSDVSSYLEGQAAKEFIAWLVKGRGRRDFPEEVAIVEELGRRHADGSFSDEMNTILDNLAARDFINWLIQTKITDRK

Approximately 19-21 kDa

Greater than 95% as determined by reducing SDS-PAGE.

溶液.

Supplied as a 0.2 μm filtered solution of 20 mM Tris-HCl, 200 mM NaCl, 1 mM DTT, 50% Glycerol, pH 8.0.

<1 EU/μg, determined by LAL method.

Stored at -80°C for 1 year. It is stable at -20°C for 3 months after opening. It is recommended to freeze aliquots at -80°C for extended storage. Avoid repeated freeze-thaw cycles.

Shipping with dry ice.

• [1]. Müller TD, et al. The New Biology and Pharmacology of Glucagon. Physiol Rev. 2017 Apr;97(2):721-766.  [Content Brief]

  [2]. Zeigerer A, et al. Glucagon's Metabolic Action in Health and Disease. Compr Physiol. 2021 Apr 1;11(2):1759-1783.  [Content Brief]

  [3]. Jiang G, et al. Glucagon and regulation of glucose metabolism. Am J Physiol Endocrinol Metab. 2003 Apr;284(4):E671-8.  [Content Brief]

  [4]. Ellingsgaard H, et al. Interleukin-6 enhances insulin secretion by increasing glucagon-like peptide-1 secretion from L cells and alpha cells. Nat Med. 2011 Oct 30;17(11):1481-9.  [Content Brief]

  [5]. https://pubmed.ncbi.nlm.nih.gov/12554744/

  [6]. Lee YS, et al. Anti-Inflammatory Effects of GLP-1-Based Therapies beyond Glucose Control. Mediators Inflamm. 2016;2016:3094642.  [Content Brief]

  [7]. Zhang Y, et al. Glucagon Potentiates Insulin Secretion Via β-Cell GCGR at Physiological Concentrations of Glucose. Cells. 2021 Sep 21;10(9):2495.  [Content Brief]

  [8]. Piro S, et al. Chronic exposure to GLP-1 increases GLP-1 synthesis and release in a pancreatic alpha cell line (α-TC1): evidence of a direct effect of GLP-1 on pancreatic alpha cells. PLoS One. 2014 Feb 28;9(2):e90093.  [Content Brief]

  [9]. The GCG protein (Human) (150 μg/kg, intraperitoneally, once daily for 5 days) can stimulate thermogenesis in brown adipose tissue in Sprague-Dawley rats^[9].
   [Content Brief]

  [10]. Åm MK, et al. Intraperitoneal and subcutaneous glucagon delivery in anaesthetized pigs: effects on circulating glucagon and glucose levels. Sci Rep. 2020 Aug 13;10(1):13735.  [Content Brief]