glucagon , human

Glucagon is a 29-amino-acid peptide hormone liberated in the alpha cells of the islets of Langerhans. Glucagon-producing alpha cells represent one of the earliest populations of detectable islet cells in the developing endocrine pancreas.

Glucagon 对蛋白质和氨基酸的代谢产生显著的调节作用。它抑制了氨基酸与肝脏、肌肉以及胰腺蛋白的结合，增加氮的排出，并促进肝脏内尿素的合成。同时，Glucagon 增加了肝脏中转氨酶和尿素循环酶的浓度，提高了肝脏对氨基酸的摄取，并加强了氨基酸与肝糖原之间的结合，从而降低了血液中的氨基酸浓度。

Glucagon-Like Peptide 1 (GLP-1) (7-36)-Lys (Biotin), amide, human 是一种被 C 端标记的生物素化 GLP-1(7-36) 酰胺。

Human glucagon-like peptide-1-(7-36)-Lys(Biotin) amide 是一种带有生物素标签的Glucagon-like peptide-1-(7-36)，后者为一种具备提升胰岛素释放功能，从而表现出抗糖尿病活性的胃肠道肽。

Biotinyl-Glucagon (1-29), human, bovine, porcine 为带生物素标记的Glucagon衍生物，此肽类激素由胰腺α细胞分泌，功能是提升血液中的葡萄糖与脂肪酸浓度。

'(Met(O)27)-Glucagon (1-29) (human, rat, porcine) 为修饰版胰高血糖素。在大鼠肝细胞内，其促进葡萄糖合成的活性虽与天然胰高血糖素相似，但呈现出较低效率，暗示蛋氨酸对于胰高血糖素与其肝脏受体绑定具有关键性作用。'

'(Asp28)-Glucagon (1-29) (human, rat, porcine)' 为胰高血糖素的一种改良型结构，在第28位氨基酸残基上天冬氨酸（Asp）替换原有残基，显著提高了该化合物在生理pH条件下的溶解性，且保持了与天然胰高血糖素相同的生物活性。

Glucagon-like peptide 1 (1-37), human (TFA), is a highly potent agonist of the GLP-1 receptor and is a pancreatic hormone synthesized through post-translational processing of proglucagon.

Glucagon-like peptide 1 (1-37), human, is a highly potent agonist of the GLP-1 receptor and a pancreatic hormone synthesized through post-translational processing of proglucagon. Unlike truncated forms of GLP-1, it has no effect on food intake in rats.

Glucagon-like peptide 1 (1-37), human acetate 是一种高效的 GLP-1 受体激动剂。

Glucagon-like peptide 2 (GLP-2) is a recently identified intestinal epithelium-specific growth factor that has been shown to reduce the severity of inflammatory disorders of the intestine in rodent models. Currently Glucagon-Like Peptide 2 is used as a po

Glucagon (19-29), human acetate 是一种从胰高血糖素加工而来的 COOH 末端片段，是一种有效的胰岛素分泌抑制剂。

Semaglutide 是人胰高血糖素样肽-1受体激动剂，是一种人胰高血糖素样肽-1 的长效类似物。它有用于 2 型糖尿病研究的潜力。

GLP-1R Agonist DMB 是胰高血糖素样肽1受体的激动剂（GLP-1R；重组人受体的 KB＝26.3nM）。

Glucagon (1-29), bovine, human, porcine 是由胰腺 α 细胞产生的一种具有胰高血糖素活性的激素，可促进糖原分解和糖异生化，可用于研究肥胖和糖尿病。

Glucagon (1-29), bovine, human, porcine hydrochloride 是一种由胰腺 α 细胞产生的多肽激素。它可激活 HNF4α 并促进 HNF4α 磷酸化，促进糖异生。

ECC5004是激活GLP-1R(GLP-1受体)的化学物质。此化合物在HEK293细胞系中（这些细胞表达了人类GLP-1R），能诱导cAMP的积累，其有效浓度中值（EC50）低于20 nM。

ZP3022是一种兼具glucagon-like peptide 1 receptor (GLP-1R)和cholecystokinin 2 (CCK2) receptor的激动剂。它在表达GLP-1R或CCK2 receptor的HEK293细胞中，选择性增加cAMP积累或ERK磷酸化，而在表达CCK1 receptor的HEK293细胞中，该作用较弱（人类受体的EC50分别为0.02, 10.3和>1,000 nM）。ZP3022（40 nM）在体外实验中促进大鼠新生β细胞的增殖，并在大鼠胰岛中以10和100 nM浓度应用时增强葡萄糖诱导的胰岛素分泌（GSIS），同时以40 nmol/kg剂量每日两次给药可减少大鼠体重。在db/db小鼠中，每日100 nmol/kg剂量的ZP3022增加β细胞和胰腺总体积，同时改善葡萄糖耐量。此外，它在db/db小鼠中降低食物摄入量，但不影响体重。

NVP-DPP728 是一种有效、可逆、腈依赖性二肽基肽酶 IV (DPP-IV)抑制剂，Ki 值为 11 nM。NVP-DPP728 可抑制胰高血糖素样肽-1 (GLP-1)的降解，从而增强响应于葡萄糖摄入的胰岛素释放。NVP-DPP728 可用于糖尿病研究。

L-168049 是一种选择性和非竞争性人胰高血糖素受体拮抗剂，对人、鼠和犬的 IC50 分别为 3.7 nM、63 nM 和 60 nM。

GRA Ex-25 (GRA-Ex-25) 是glucagon 受体抑制剂，其对大鼠和人的 glucagon 受体的IC50值分别为 56 和 55 nM。

Skyrin是一种天然的双蒽醌衍生物和受体选择性的胰高血糖素拮抗剂，抑制HeLa、Vero、K562、Raji、Wish和Calu-1肿瘤细胞系的生长。

GLP-1 amide is a peptide hormone cleaved from proglucagon in the pancreas.1,2 Mice lacking the glucagon receptor (Gcgr- -) have approximately nine-fold higher levels of total GLP-1 amide, including GLP-1 (1-36) amide and truncated GLP-1 (7-36) amide , in pancreatic tissue compared to wild-type mice.2References1. Schjoldager, B.T., Mortensen, P.E., Christiansen, J., et al. GLP-1 (glucagon-like peptide 1) and truncated GLP-1, fragments of human proglucagon, inhibit gastric acid secretion in humans. Dig. Dis. Sci. 34(5), 703-708 (1989).2. Gelling, R.W., Du, X.Q., Dichmann, D.S., et al. Lower blood glucose, hyperglucagonemia, and pancreatic α cell hyperplasia in glucagon receptor knockout mice. Proc. Natl. Acad. Sci. U.S.A. 100(3), 1438-1443 (2003). GLP-1 amide is a peptide hormone cleaved from proglucagon in the pancreas.1,2 Mice lacking the glucagon receptor (Gcgr- -) have approximately nine-fold higher levels of total GLP-1 amide, including GLP-1 (1-36) amide and truncated GLP-1 (7-36) amide , in pancreatic tissue compared to wild-type mice.2 References1. Schjoldager, B.T., Mortensen, P.E., Christiansen, J., et al. GLP-1 (glucagon-like peptide 1) and truncated GLP-1, fragments of human proglucagon, inhibit gastric acid secretion in humans. Dig. Dis. Sci. 34(5), 703-708 (1989).2. Gelling, R.W., Du, X.Q., Dichmann, D.S., et al. Lower blood glucose, hyperglucagonemia, and pancreatic α cell hyperplasia in glucagon receptor knockout mice. Proc. Natl. Acad. Sci. U.S.A. 100(3), 1438-1443 (2003).

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.