Glucagon Receptor
Glucagon is a 29-amino acid polypeptide secreted by the alpha or glucagon cell of the islet of Langerhans in response to hypoglycemia, arginine, gastric inhibitory polypeptide (during ambient reduced glucose levels), gastrin, and potassium chloride. Glucagon action is transduced by a G-protein-coupled receptor (GCGR/Gcgr) that is a member of the class II GCGR superfamily of seven transmembrane spanning receptors that are coupled via GTP-binding proteins to adenyl cyclase resulting in an increase in cAMP production. cAMP activates signaling pathways that cause an increase in gluconeogenesis, glycogenolysis, and fatty acid oxidation. In addition, glucagon controls glucose, energy, and lipid metabolism at least in part via AC/cAMP independent signals including p38MAPK, IP3/DAG/Ca, peroxisome proliferator-activated receptor-α (PPARα) and fibroblast growth factor 21 (FGF21)-dependent pathways. Binding sites for glucagon have been identified in liver, kidney, intestinal smooth muscle, brain, adipose tissue, heart, pancreatic islet beta cells and placenta. Gcgr expression is positively regulated by glucose and negatively regulated by glucagon and agents that increase intracellular cAMP.
References
1.Charron MJ,et al. J Endocrinol. 2015;224(3):R123–R130.
References
1.Charron MJ,et al. J Endocrinol. 2015;224(3):R123–R130.
GPCR/G Protein
ACAT(3)
Angiotensin Receptor(27)
Antibacterial(545)
Bombesin Receptor(13)
Bradykinin Receptor(23)
Calcium Channel(197)
cAMP(16)
Cannabinoid Receptor(88)
CaSR(18)
CGRP Receptor(18)
Chemokine Receptor(104)
Cholecystokinin Receptor(24)
CRF Receptor(15)
Dopamine Receptor(182)
Endothelin Receptor(28)
FFAR(5)
Galanin Receptor(1)
GHSR(20)
Glucagon Receptor(51)
GPCR19(9)
GPR119(3)
Hedgehog (Hh)(35)
Histamine Receptor(139)
Imidazoline Receptor(1)
Leukotriene Receptor(15)
LHR(1)
LPA Receptor(19)
Lysophospholipid Receptor(13)
mAChR(25)
MCHR(8)
Melanocortin Receptor(28)
Melatonin Receptor(7)
Motilin Receptor(4)
Neurokinin Receptor(43)
Neuropeptide Y Receptor(44)
Neurotensin Receptor(11)
Orexin Receptor(16)
Other Targets(3)
OXTR(2)
P2Y Receptor(14)
PAR(28)
Platelet-activating Factor Receptor(2)
Prostaglandin Receptor(79)
PTH Receptor(1)
S1P Receptor(35)
SGLT(26)
Somatostatin Receptor(16)
Urotensin Receptor(4)
Vasopressin Receptor(20)
Glucagon Receptor
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Avexitide acetate
产品货号 : M37916
cas no: 2051593-46-3
Avexitide acetate (exendin 9-39) is a potent glucagon-like peptide 1 receptor (GLP-1R) antagonist for the study of post-obesity hypoglycemia. -
Lotiglipron
产品货号 : M37118
cas no: 2401892-75-7
Lotiglipron (PF-07081532) 是一种具有口服活性的 GLP-1R 激动剂。Lotiglipron 可降低血糖和体重,可用于 2 型糖尿病 (T2DM) 的研究。 -
Survodutide
产品货号 : M36653
cas no: 2805997-46-8
Survodutide (BI 456906) 是一种有效的、选择性的胰高血糖素受体/GLP-1 受体 (GCGR/GLP-1R) 双重激动剂,在 CHO-K1 细胞中的 EC50 值分别为 0.52 nM 和 0.33 nM。Survodutide 是一种 29 个氨基酸的肽,是含有 C18 脂肪酸的有效酰化肽。Survodutide 通过增加能量消耗和减少食物摄入来实现强大的抗肥胖功效。 -
Retatrutide
产品货号 : M36652
cas no: 2381089-83-2
Retatrutide (LY3437943) 是胰高血糖素受体 (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) 的三重激动剂肽。Retatrutide 结合人 GCGR、GIPR 和 GLP-1R,EC50 值分别为 5.79、0.0643 和 0.775 nM。Retatrutide 可用于肥胖的研究。 -
GLP-1R agonist 3
产品货号 : M35751
cas no: 2428640-18-8
GLP-1R agonist 3 是一种有效的 GLP-1R 激动剂。GLP-1R agonist 3 是一种增稠的咪唑衍生物化合物。胰高血糖素样肽-1 (GLP-1) 是一种由下消化道 L 细胞分泌的肠道降血糖激素。GLP-1R agonist 3 具有糖尿病研究潜力 (摘自专利 WO2021197464A1,化合物 1)。