human glucagon receptor

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。

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。

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）。

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。

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。

Skyrin is a fungal metabolite characterized by a bisanthraquinone structure. It interferes with glucagon signaling through adenylate cyclase without binding to the glucagon receptor. At 10 μM, skyrin reduces both glucagon-stimulated cAMP production and glycogenolysis. It does not interfere with epinephrine or glucagon-like peptide 1 effects on these parameters.[1] Reference：[1]. Parker, J.C., McPherson, R.K., Andrews, K.M., et al. Effects of skyrin, a receptor-selective glucagon antagonist, in rat and human hepatocytes. Diabetes 49, 2079-2086 (2012).

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.

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 为人源化IgG2κ类抗体，专一性靶向GLP1R（胰高血糖素样肽1受体）。

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。

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。

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。