Page last updated: 2024-11-13

ly2409021

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

adomeglivant: a glucagon receptor antagonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID91933867
CHEMBL ID3707351
MeSH IDM000610534

Synonyms (29)

Synonym
1488363-78-5
adomeglivant, (-)-
ly-2409021
3-(4-((1s)-1-((4'-tert-butyl-2,6-dimethylbiphenyl-4-yl)oxy)-4,4,4- trifluorobutyl)benzamido)propanoic acid
adomeglivant [who-dd]
.beta.-alanine, n-(4-((1s)-1-((4'-(1,1-dimethylethyl)-2,6-dimethyl(1,1'-biphenyl)-4-yl)oxy)-4,4,4-trifluorobutyl)benzoyl)-
adomeglivant [usan]
adomeglivant [inn]
adomeglivant
74Z5ZL2KVG ,
ly2409021
CHEMBL3707351
unii-74z5zl2kvg
ly 2409021
CS-5729
HY-19904
3-[[4-[(1s)-1-[4-(4-tert-butylphenyl)-3,5-dimethylphenoxy]-4,4,4-trifluorobutyl]benzoyl]amino]propanoic acid
gtpl9479
adomeglivant (usan)
D10861
DB11704
(s)-3-(4-(1-(4'-tert-butyl-2,6-dimethylbiphenyl-4-yloxy)-4,4,4-trifluorobutyl)benzamido)propanoic acid
Q27266313
3-(4-{(1s)-1-[(4'-tert-butyl-2,6-dimethylbiphenyl-4-yl)oxy]-4,4,4-trifluorobutyl}benzamido)propanoic acid
A858152
F85410
MS-30128
fasltmsupqdlib-mhzltwqesa-n
AKOS040741049

Research Excerpts

Treatment

ExcerptReferenceRelevance
"LY2409021 treatment showed significant HbA1c reductions vs placebo (LS mean difference -0.77%; Pā€‰<ā€‰.001) but not sitagliptin (-0.20%; Pā€‰=ā€‰.383)."( Treatment with LY2409021, a glucagon receptor antagonist, increases liver fat in patients with type 2 diabetes.
Chalasani, N; Garhyan, P; Guzman, CB; Hardy, TA; Kazda, C; Liu, R; Pillai, SG; Regev, A; Shankar, S; Zhang, XM, 2017
)
1.53

Dosage Studied

ExcerptRelevanceReference
" Serum aminotransferases increased in a dose-dependent manner with multiple dosing and reversed after cessation of dosing."( Short-term administration of the glucagon receptor antagonist LY2409021 lowers blood glucose in healthy people and in those with type 2 diabetes.
Deeg, MA; Fu, H; Garhyan, P; Kelly, RP; Lim, CN; Loh, MT; Pinaire, JA; Prince, MJ; Raddad, E, 2015
)
0.66
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (2)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
PPM1D proteinHomo sapiens (human)Potency26.21230.00529.466132.9993AID1347411
Interferon betaHomo sapiens (human)Potency26.21230.00339.158239.8107AID1347411
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (30)

Processvia Protein(s)Taxonomy
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (5)

Processvia Protein(s)Taxonomy
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (2)

Processvia Protein(s)Taxonomy
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (4)

Assay IDTitleYearJournalArticle
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1345985Human glucagon receptor (Glucagon receptor family)2016Diabetes care, Jul, Volume: 39, Issue:7
Evaluation of Efficacy and Safety of the Glucagon Receptor Antagonist LY2409021 in Patients With Type 2 Diabetes: 12- and 24-Week Phase 2 Studies.
AID1345985Human glucagon receptor (Glucagon receptor family)2015Diabetes, obesity & metabolism, Apr, Volume: 17, Issue:4
Short-term administration of the glucagon receptor antagonist LY2409021 lowers blood glucose in healthy people and in those with type 2 diabetes.
AID1418649Antihyperglycemic activity in db/db mouse assessed as reduction in blood glucose level at 50 mg/kg, po administered once per day for 4 weeks and measured after 12 hrs fasting2018Bioorganic & medicinal chemistry, 11-15, Volume: 26, Issue:21
Design, synthesis, and effects of novel phenylpyrimidines as glucagon receptor antagonists.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (13)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's9 (69.23)24.3611
2020's4 (30.77)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 20.87

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index20.87 (24.57)
Research Supply Index3.00 (2.92)
Research Growth Index4.57 (4.65)
Search Engine Demand Index18.60 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (20.87)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials6 (46.15%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other7 (53.85%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]