human glucagon receptor

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。

NNC-0640 是人类胰高血糖素受体阴性变构调节剂(IC50:69.2 nM)。

Semaglutide 是一种长效、选择性、竞争型 GLP-1R 激动剂，是一种人胰高血糖素样肽-1 的长效类似物，具有强效降糖、减重、心血管保护、神经保护等活性。Semaglutide 激活 GLP-1R 后促进胰岛素分泌、抑制胃排空和食欲，同时通过增强自噬、抑制氧化应激和凋亡。Semaglutide 还参与调节线粒体功能及脂质代谢。Semaglutide 可用于 2 型糖尿病、肥胖症、帕金森病、代谢相关脂肪性肝病 (MASLD) 等神经退行性疾病和肝脏疾病，以及癌症的研究。

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。

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.

Glucagon receptor antagonist I is a competitive antagonist of the glucagon receptor (GCGR; IC50 = 181 nM). It blocks glucagon-induced glycogenolysis in primary human hepatocytes and isolated liver. Glucagon receptor antagonist I, at 50 mg/kg, reduces the increase in glucose levels observed after intraperitoneal administration of glucagon in humanized mice. Glucagon receptor antagonist inactive control does not prevent glucagon-mediated actions.

GLP-1(7-36), amide (MKC 253) 是一种生理性肠降血糖素，能够刺激胰岛素分泌。

GCGR antagonist2 是一种呋喃-2-碳酰肼化合物，是具有口服活性的胰高血糖素受体拮抗剂。GCGR antagonist2 与 hGluR 结合的 Kd 值为 2.3 nM，抑制大鼠受体的 IC50值为 0.43 nM。GCGR antagonist2 可抑制胰高血糖素刺激的糖原分解。

Albiglutide TFA 是一种胰高血糖素样肽GLP-1模拟物，是长效的GLP-1受体激动剂。Albiglutide TFA 可显著降低糖化血红蛋白 (A1C)。Albiglutide TFA 可用于研究 2 型糖尿病 (T2D)。Albiglutide TFA 是由抗DPP-4的GLP-1二聚体与人白蛋白的基因融合产生的。

GLP-1(9-36)amide TFA, 作为胰高血糖素样肽-1 (7-36)amide的主要代谢产物，是人胰腺GLP-1受体的拮抗剂。

Retatrutide (LY3437943) acetate 是一种针对胰高血糖素受体（GCGR）、葡萄糖依赖性促胰岛素多肽受体（GIPR）和胰高血糖素样肽-1 受体（GLP-1R）的三重肽激动剂。该化合物能有效抑制这三种受体，其EC50值分别为GCGR 5.79 nM、GIPR 0.0643 nM和GLP-1R 0.775 nM，是肥胖研究领域的潜在工具。

Gulgafafusp alfa是一种人源化的单克隆抗体，专一性靶向GLP1R(胰高血糖素样肽1受体)。

Tirzepatide sodium是一种双重胰高血糖素样肽-1（GLP-1）和葡萄糖依赖性促胰岛素多肽（GIP）受体激动剂肽类药物的钠盐形式，可通过同时激活GIP和GLP-1受体增强胰岛素分泌并改善血糖控制。Tirzepatide sodium表现出降低体重和改善代谢参数的作用，被用于2型糖尿病及代谢性疾病相关研究。

5(S)-HEPE, an active metabolite of eicosapentaenoic acid (EPA), is produced via the action of 5-lipoxygenase (5-LO). This compound functions as an agonist for G protein-coupled receptor 119 (GPR119), promoting cAMP accumulation in CHO-K1 cells expressing human GPR119 at 10 µM concentration. Additionally, 5(S)-HEPE enhances glucose-stimulated insulin secretion from MING6 insulinoma pancreatic islets and glucagon-like peptide 1 (GLP-1) secretion from HuTu 80 adenocarcinoma cells at the same concentration. Notably, serum levels of 5(S)-HEPE are increased in hyperlipidemia patients.

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。