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GCGR

Brief Information

Name:Glucagon receptor
Target Synonym:GL-R,GCGR,Glucagon Receptor,GGR,Receptors, Glucagon
Number of Launched Drugs:5
Number of Drugs in Clinical Trials:33
Lastest Research Phase:Approved

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Part of Bioactivity data

CHEK-ATF103-Cell-based assay
 GCGR FACS

Expression analysis of human GCGR on Human GCGR (Luc) HEK293 Reporter Cell by FACS.
Cell surface staining was performed on Human GCGR (Luc) HEK293 Reporter Cell or negative control cell using Alexa Fluor® 488-labeled anti-human GCGR antibody.

GCR-H53H3-SPR
 GCGR SPR

Human GCGR Protein, Fc Tag (Cat. No. GCR-H53H3) immobilized on CM5 Chip can bind GLP-1 (7-37) with an affinity constant of 51.1 μM as determined in a SPR assay (Biacore 8K) (Routinely tested).

GCR-H82E3-SPR
 GCGR SPR

Biotinylated Human GCGR Protein, His,Avitag (Cat. No. GCR-H82E3) immobilized on CM5 Chip can bind GLP-1 (7-37) with an affinity constant of 48.5 μM as determined in a SPR assay (Biacore 8K) (QC tested).

Synonym Name

Glucagon R, GCGR,Glucagon receptor

Background

G-protein coupled receptor for glucagon that plays a central role in the regulation of blood glucose levels and glucose homeostasis. Regulates the rate of hepatic glucose production by promoting glycogen hydrolysis and gluconeogenesis. Plays an important role in mediating the responses to fasting. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Promotes activation of adenylate cyclase. Besides, plays a role in signaling via a phosphatidylinositol-calcium second messenger system.

Clinical and Translational Updates

Public Drug Information

Name Research Code Research Phase Company First Brand Name First Approved Country First Indication First Approved Company First Approved Date Indications Clinical Trials
Glucagon (rDNA origin, Novo Nordisk) GL-G Approved Novo Nordisk A/S GlucaGen, Glucagon G United States Gastrointestinal Diseases; Hypoglycemia Novo Nordisk A/S 1998-06-22 Diabetes Mellitus, Type 1; Gastrointestinal Diseases; Hypoglycemia; Obesity Details
Dasiglucagon ZP-GA-1; ZP-4207 Approved Zealand Pharma A/S Zegalogue United States Hypoglycemia Zealand Pharma Us Inc 2021-03-22 Diabetes Mellitus, Type 1; Congenital Hyperinsulinism; Hypoglycemia; Glucose Metabolism Disorders; Hyperinsulinism Details
Glucagon MP-123456B Approved Eli Lilly And Company Ogluo, Baqsimi EU Hypoglycemia Eli Lilly Nederland BV 1960-11-14 Diabetes Mellitus, Type 1; Diabetes Mellitus, Type 2; Hypoglycemia Details
Glucagon intranasal (Eli Lilly/Locemia Solutions) AMG504-1; LY-900018 Approved Amg Medical, Locemia Solutions Diabetes Mellitus, Type 1; Diabetes Mellitus, Type 2; Hypoglycemia; Diabetes Mellitus Details
Glucagon (Xeris Pharmaceuticals) Approved Xeris Pharmaceuticals Inc Gvoke United States Hypoglycemia null 1960-01-01 Hypoglycemia; Hyperinsulinism Details

Clinical Drug Information

Name Research Code Research Phase Company Indications Clinical Trials
PRT-001 PRT-001 Phase 3 Clinical Particle Therapeutics Hypoglycemia Details
Retatrutide LY-3437943 Phase 3 Clinical Eli Lilly And Company Diabetes Mellitus, Type 2; Renal Insufficiency; Sleep Apnea, Obstructive; Osteoarthritis, Knee; Cardiovascular Diseases; Hepatic Insufficiency; Obesity; Arthralgia; Renal Insufficiency, Chronic; Overweight; Kidney Failure, Chronic Details
Survodutide BI-456906; BI-456909 Phase 3 Clinical Zealand Pharma A/S Diabetes Mellitus, Type 2; Metabolic Dysfunction-Associated Steatotic Liver Disease; Liver Cirrhosis; Liver Diseases; Obesity; Overweight; Diabetes Mellitus Details
Pemvidutide ALT-801(Altimmune); SP-1373; VPD-107 Phase 2 Clinical Velocity Pharmaceutical Development Metabolic Dysfunction-Associated Steatotic Liver Disease; Diabetes Mellitus, Type 2; Obesity; Overweight Details
Efinopegdutide JNJ-64565111; HM-12525A; JNJ-5111; MK-6024 Phase 2 Clinical Hanmi Pharmaceutical Co Ltd Metabolic Dysfunction-Associated Steatotic Liver Disease; Diabetes Mellitus, Type 2; Hepatic Insufficiency; Obesity; Kidney Failure, Chronic Details
Efocipegtrutide HM-15211 Phase 2 Clinical Hanmi Pharmaceutical Co Ltd Metabolic Dysfunction-Associated Steatotic Liver Disease; Obesity Details
volagidemab AMG-477; REMD-477 Phase 2 Clinical Amgen Inc Diabetes Mellitus, Type 1; Diabetes Mellitus, Type 2; Glucose Intolerance; Insulin Resistance; Hyperglycemia; Diabetes Mellitus Details
Isosteviol ISV; STX-03 Phase 2 Clinical Stevia Pharma Diabetes Mellitus, Type 2 Details
Oxyntomodulin long-acting (Pharmsynthez/Xenetic Biosciences) Phase 2 Clinical Pharmsynthez, Xenetic Biosciences Inc Diabetes Mellitus, Type 2; Obesity Details
Pegapamodutide WG4ID2U7FT; TT-401; LY-2944876; OPK-88003 Phase 2 Clinical Eli Lilly And Company Diabetes Mellitus, Type 2; Obesity Details
IONIS-GCGRRx IONIS-GCGRRx; ISIS-449884; ISISGCGRRx Phase 2 Clinical Ionis Pharmaceuticals Inc Diabetes Mellitus, Type 2 Details
Efpegerglucagon HM-15136 Phase 2 Clinical Hanmi Pharmaceutical Co Ltd Congenital Hyperinsulinism; Diabetes Mellitus, Type 2 Details
AZD9550 AZD9550; AZD-9550 Phase 2 Clinical Astrazeneca Plc Metabolic Dysfunction-Associated Steatotic Liver Disease Details
MWN-101 MWN-101 Phase 2 Clinical Shanghai Minwei Biotechnology Co Ltd Diabetes Mellitus, Type 2; Obesity; Overweight Details
RBD-4988 RBD-4988 Phase 2 Clinical Suzhou Ribo Life Science Co Ltd Diabetes Mellitus, Type 2 Details
PB-718 PB-718 Phase 2 Clinical Peg Bio Co Ltd Congenital Hyperinsulinism; Metabolic Dysfunction-Associated Steatotic Liver Disease; Obesity; Overweight Details
Cotadutide MEDI-0382 Phase 2 Clinical Medimmune Llc Diabetes Mellitus, Type 2; Metabolic Dysfunction-Associated Steatotic Liver Disease; Renal Insufficiency; Liver Cirrhosis; Hepatic Insufficiency; Diabetic Nephropathies; Renal Insufficiency, Chronic; Obesity; Diabetes Mellitus Details
NN-9277 NN-9277; NNC-9204-1177 Phase 1 Clinical Novo Nordisk A/S Obesity; Overweight; Nutritional and Metabolic Diseases Details
Glucagon (rDNA origin, Lilly) Phase 1 Clinical Eli Lilly And Company Diabetes Mellitus, Type 1; Hypoglycemia; Insulin Resistance; Obesity Details
Glucagon (Translational Research Institute for Metabolism and Diabetes, Florida) Phase 1 Clinical Translational Research Institute For Metabolism And Diabetes Obesity Details
NNC-92041706 NNC9204-1706; NNC-92041706; NN-9423; NNC-92041706-A Phase 1 Clinical Novo Nordisk A/S Obesity; Nutritional and Metabolic Diseases Details
PRT-003 PRT-003 Phase 1 Clinical Particle Therapeutics Details
SAR-441255 SAR-441255 Phase 1 Clinical Sanofi Overweight Details
Glucagon/insulin human(Abvance Therapeutics) ABV-100 Phase 1 Clinical Abvance Therapeutics Hypoglycemia Details
PB-722 PB722; PB-722 Phase 1 Clinical Peg Bio Co Ltd Congenital Hyperinsulinism Details
UBT-251 UBT-251; UBT251 Phase 1 Clinical Lianbang Biotechnology (Zhuhai Hengqin) Co Ltd Metabolic Dysfunction-Associated Steatotic Liver Disease; Diabetes Mellitus, Type 2; Obesity; Overweight Details
TY-751 TY-751; TY751 Phase 1 Clinical Tianjin Remedy Research Institute Metabolic Dysfunction-Associated Steatotic Liver Disease; Diabetes Mellitus, Type 2; Obesity; Diabetes Mellitus Details
DA-1726 DA-1726 Phase 1 Clinical Dong-A ST Co Ltd Metabolic Dysfunction-Associated Steatotic Liver Disease; Obesity Details
DR-10624 DR-10624 Phase 1 Clinical Zhejiang Doer Biologics Corp Hypertriglyceridemia; Diabetes Mellitus, Type 2; Metabolic Dysfunction-Associated Steatotic Liver Disease; Metabolic Syndrome; Obesity; Overweight; Diabetes Mellitus Details
TB-001 TB-001; TB001 Phase 1 Clinical Shenzhen Tuwei Anchuang Technology Development Co Ltd Metabolic Dysfunction-Associated Steatotic Liver Disease; Liver Cirrhosis Details
Human glucagon(Shanghai Duomirui) Phase 1 Clinical Shanghai Duomirui Biotechnology Co Ltd Hypoglycemia Details
DD-01 DD-01 Phase 1 Clinical Neuraly Inc, D&D Pharmatech Metabolic Dysfunction-Associated Steatotic Liver Disease; Diabetes Mellitus, Type 2; Obesity; Overweight Details

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