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GCGR

概要

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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生物活性データの一部

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

公開薬物情報

Name Research Code Research Phase Company First Brand Name First Approved Country First Indication First Approved Company First Approved Date Indications Clinical Trials
Glucagon intranasal (Eli Lilly/Locemia Solutions) AMG504-1; LY-900018 Approved Amg Medical, Locemia Solutions Hypoglycemia Details
Glucagon (rDNA origin, Novo Nordisk) GL-G Approved Novo Nordisk A/S GlucaGen, Glucagon G Japan Hypoglycemia Novo Nordisk A/S 1998-06-22 Diabetes Mellitus, Type 1; Hypoglycemia; Obesity Details
Glucagon (Xeris Pharmaceuticals) Approved Xeris Pharmaceuticals Inc Gvoke United States Hypoglycemia Xeris Pharmaceuticals Inc 1960-01-01 Hypoglycemia; Hyperinsulinism Details
Glucagon (rDNA origin, Lilly) Approved Eli Lilly And Company Glucagon United States Hypoglycemia Eli Lilly And Company 1998-09-11 Diabetes Mellitus, Type 1; Hypoglycemia; Insulin Resistance; Obesity Details
Glucagon MP-123456B Approved Eli Lilly And Company Baqsimi, Ogluo EU Hypoglycemia Eli Lilly Nederland BV 1960-11-14 Diabetes Mellitus, Type 1; Diabetes Mellitus, Type 2; Hypoglycemia Details
Dasiglucagon ZP-GA-1; ZP-4207 Approved Zealand Pharma A/S Zegalogue United States Hypoglycemia Zealand Pharma Us Inc 2021-03-22 Congenital Hyperinsulinism; Diabetes Mellitus, Type 1; Hypoglycemia; Hyperinsulinism; Glucose Metabolism Disorders Details

臨床試験情報

Name Research Code Research Phase Company Indications Clinical Trials
PRT-001 PRT-001 Phase 3 Clinical Particle Therapeutics Hypoglycemia Details
PRT-003 PRT-003 Phase 1 Clinical Particle Therapeutics Details
Isosteviol ISV; STX-03 Phase 2 Clinical Stevia Pharma Diabetes Mellitus, Type 2 Details
Human glucagon(Shanghai Duomirui) Phase 1 Clinical Shanghai Duomirui Biotechnology Co Ltd Hypoglycemia Details
ISIS-325568 ISIS-325568 Ionis Pharmaceuticals Inc Details
MK-3577 MK-3577 Merck Sharp & Dohme Corp Details
IONIS-GCGRRx IONIS-GCGRRx; ISIS-449884; ISISGCGRRx Phase 2 Clinical Ionis Pharmaceuticals Inc Diabetes Mellitus, Type 2 Details
Bamadutide SAR-425899 Sanofi Details
MK-0893 MK-0893; L-001241689 Merck & Co Inc Details
PF-06291874 PF-6291874; PF-06291874 Pfizer Inc Details
MK-5823 MK-5823 Merck Sharp & Dohme Corp Details
MK-8521 MK-8521 Merck Sharp & Dohme Corp Details
LGD-6972 LGD-6972; MB-11262; RVT-1502 Ligand Pharmaceuticals Inc Details
Glucagon biosimilar (Hospira) Hospira Details
BioChaperone Glucagon BC Glucagon Adocia Details
Efocipegtrutide HM-15211 Phase 2 Clinical Hanmi Pharmaceutical Co Ltd Non-alcoholic Fatty Liver Disease; Obesity Details
Oxyntomodulin long-acting (Pharmsynthez/Xenetic Biosciences) Phase 2 Clinical Pharmsynthez, Xenetic Biosciences Inc Diabetes Mellitus, Type 2; Obesity Details
Glucagon (Translational Research Institute for Metabolism and Diabetes, Florida) Phase 1 Clinical Translational Research Institute For Metabolism And Diabetes Obesity Details
BI-456906 BI-456906 Phase 2 Clinical Zealand Pharma A/S Non-alcoholic Fatty Liver Disease; Diabetes Mellitus, Type 2; Liver Cirrhosis; Liver Diseases; Obesity; Overweight Details
DR-10624 DR-10624 Phase 1 Clinical Zhejiang Doer Biologics Corp Diabetes Mellitus, Type 2; Non-alcoholic Fatty Liver Disease; Metabolic Syndrome; Obesity; Diabetes Mellitus Details
Pemvidutide ALT-801(Altimmune); SP-1373; VPD-107 Phase 2 Clinical Velocity Pharmaceutical Development Non-alcoholic Fatty Liver Disease; Diabetes Mellitus, Type 2; Obesity; Overweight Details
RBD-4988 RBD-4988 Phase 2 Clinical Suzhou Ruibo Biological Technology Co Ltd Diabetes Mellitus, Type 2 Details
Efinopegdutide JNJ-64565111; HM-12525A; JNJ-5111; MK-6024 Phase 2 Clinical Hanmi Pharmaceutical Co Ltd Diabetes Mellitus, Type 2; Non-alcoholic Fatty Liver Disease; Obesity; Kidney Failure, Chronic Details
HM-15136 HM-15136 Phase 2 Clinical Hanmi Pharmaceutical Co Ltd Congenital Hyperinsulinism; Diabetes Mellitus, Type 2 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
TB-001 TB001; TB-001 Phase 1 Clinical Shenzhen Tuwei Anchuang Technology Development Co Ltd Non-alcoholic Fatty Liver Disease; Liver Cirrhosis Details
Cotadutide MEDI-0382 Phase 3 Clinical Medimmune Llc Non-alcoholic Fatty Liver Disease; Diabetes Mellitus, Type 2; Renal Insufficiency; Liver Cirrhosis; Hepatic Insufficiency; Obesity; Renal Insufficiency, Chronic; Diabetes Mellitus Details
Mazdutide OXM-3; IBI-362; LY-3305677 Phase 3 Clinical Eli Lilly And Company Diabetes Mellitus, Type 2; Obesity; Overweight Details
retatrutide LY-3437943 Phase 2 Clinical Eli Lilly And Company Diabetes Mellitus, Type 2; Renal Insufficiency; Obesity; Overweight Details
DD-01 DD-01 Phase 1 Clinical Neuraly Inc, D&D Pharmatech Non-alcoholic Fatty Liver Disease; Diabetes Mellitus, Type 2; Obesity; Overweight Details
PB-718 PB-718 Phase 1 Clinical Peg Bio Co Ltd Non-alcoholic Fatty Liver Disease; Obesity Details

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