Page last updated: 2024-11-12

rm-493

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

Description

setmelanotide: an anti-obesity agent [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID11993702
CHEMBL ID3301624
SCHEMBL ID21840385
MeSH IDM000608461

Synonyms (30)

Synonym
setmelanotide [usan]
setmelanotide [who-dd]
setmelanotide [inn]
CHEMBL3301624
setmelanotide [usan:inn]
n2-acetyl-l-arginyl-l-cysteinyl-d-alanyl-l-histidyl-d-phenylalanyl-l-arginyl-l-tryptophyl-l-cysteinamide, cyclic (2-8)-disulfide
n7t15v1fuy ,
920014-72-8
l-cysteinamide, n2-acetyl-l-arginyl-l-cysteinyl-d-alanyl-l-histidyl-d-phenylalanyl-l-arginyl-l-tryptophyl-, cyclic (2->8)-disulfide
unii-n7t15v1fuy
setmelanotide
rm-493
bim-22493
gtpl9272
(4r,7s,10s,13r,16s,19r,22r)-22-[[(2s)-2-acetamido-5-(diaminomethylideneamino)pentanoyl]amino]-13-benzyl-10-[3-(diaminomethylideneamino)propyl]-16-(1h-imidazol-5-ylmethyl)-7-(1h-indol-3-ylmethyl)-19-methyl-6,9,12,15,18,21-hexaoxo-1,2-dithia-5,8,11,14,17,20
irc-022493
HY-19870
CS-6399
DB11700
1504602-49-6
Q21098917
setmelanotide acetate
rm-493; bim-22493; irc-022493
AT23144
SCHEMBL21840385
EX-A5542
setmelanotide (rm-493)
setmelanotidum
setmelanotida
bdbm50581319

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" The most common adverse events were injection site reaction and hyperpigmentation, which were reported in all ten participants in the POMC trial; nausea was reported in five participants and vomiting in three participants."( Efficacy and safety of setmelanotide, an MC4R agonist, in individuals with severe obesity due to LEPR or POMC deficiency: single-arm, open-label, multicentre, phase 3 trials.
Argente, J; Bahm, A; Chung, WK; Clément, K; Connors, H; De Waele, K; Farooqi, IS; Gonneau-Lejeune, J; Gordon, G; Kohlsdorf, K; Kühnen, P; Poitou, C; Puder, L; Stewart, M; Swain, J; van den Akker, E; Wabitsch, M; Yuan, G, 2020
)
0.56
" The most commonly reported treatment-emergent adverse events were skin hyperpigmentation (23 [61%] of 38) and injection site erythema (18 [48%])."( Efficacy and safety of setmelanotide, a melanocortin-4 receptor agonist, in patients with Bardet-Biedl syndrome and Alström syndrome: a multicentre, randomised, double-blind, placebo-controlled, phase 3 trial with an open-label period.
Argente, J; Chung, WK; Clément, K; Dollfus, H; Forsythe, E; Haqq, AM; Haws, RM; Martos-Moreno, GÁ; Mittleman, RS; Poitou, C; Yanovski, JA; Yuan, G, 2022
)
0.72
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (4)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Melanocortin receptor 4Homo sapiens (human)Ki0.00420.00000.30864.8860AID1812562; AID1852336
Melanocortin receptor 5Homo sapiens (human)IC50 (µMol)1.88380.00091.25669.5180AID1812563; AID1852340
Melanocortin receptor 3Homo sapiens (human)Ki0.01320.00010.24522.8650AID1812561; AID1852335
Melanocyte-stimulating hormone receptorHomo sapiens (human)Ki0.00460.00000.00650.0370AID1812560; AID1852334
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Melanocortin receptor 4Homo sapiens (human)EC50 (µMol)0.00030.00000.09112.6000AID1812559; AID1812567; AID1852339
Melanocortin receptor 3Homo sapiens (human)EC50 (µMol)0.00020.00010.01270.2480AID1812558; AID1852338
Melanocyte-stimulating hormone receptorHomo sapiens (human)EC50 (µMol)0.00020.00000.00800.2280AID1812557; AID1852337
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (33)

Processvia Protein(s)Taxonomy
diet induced thermogenesisMelanocortin receptor 4Homo sapiens (human)
energy reserve metabolic processMelanocortin receptor 4Homo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayMelanocortin receptor 4Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayMelanocortin receptor 4Homo sapiens (human)
feeding behaviorMelanocortin receptor 4Homo sapiens (human)
insulin secretionMelanocortin receptor 4Homo sapiens (human)
response to insulinMelanocortin receptor 4Homo sapiens (human)
positive regulation of bone resorptionMelanocortin receptor 4Homo sapiens (human)
regulation of eating behaviorMelanocortin receptor 4Homo sapiens (human)
response to melanocyte-stimulating hormoneMelanocortin receptor 4Homo sapiens (human)
negative regulation of feeding behaviorMelanocortin receptor 4Homo sapiens (human)
regulation of grooming behaviorMelanocortin receptor 4Homo sapiens (human)
regulation of metabolic processMelanocortin receptor 4Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMelanocortin receptor 5Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayMelanocortin receptor 5Homo sapiens (human)
regulation of metabolic processMelanocortin receptor 5Homo sapiens (human)
regulation of heart rateMelanocortin receptor 3Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMelanocortin receptor 3Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayMelanocortin receptor 3Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayMelanocortin receptor 3Homo sapiens (human)
regulation of blood pressureMelanocortin receptor 3Homo sapiens (human)
circadian regulation of gene expressionMelanocortin receptor 3Homo sapiens (human)
homoiothermyMelanocortin receptor 3Homo sapiens (human)
locomotor rhythmMelanocortin receptor 3Homo sapiens (human)
sodium ion homeostasisMelanocortin receptor 3Homo sapiens (human)
regulation of feeding behaviorMelanocortin receptor 3Homo sapiens (human)
regulation of metabolic processMelanocortin receptor 3Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMelanocyte-stimulating hormone receptorHomo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayMelanocyte-stimulating hormone receptorHomo sapiens (human)
UV protectionMelanocyte-stimulating hormone receptorHomo sapiens (human)
positive regulation of protein kinase A signalingMelanocyte-stimulating hormone receptorHomo sapiens (human)
sensory perception of painMelanocyte-stimulating hormone receptorHomo sapiens (human)
negative regulation of tumor necrosis factor productionMelanocyte-stimulating hormone receptorHomo sapiens (human)
intracellular signal transductionMelanocyte-stimulating hormone receptorHomo sapiens (human)
melanin biosynthetic processMelanocyte-stimulating hormone receptorHomo sapiens (human)
pigmentationMelanocyte-stimulating hormone receptorHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIMelanocyte-stimulating hormone receptorHomo sapiens (human)
UV-damage excision repairMelanocyte-stimulating hormone receptorHomo sapiens (human)
positive regulation of protein kinase C signalingMelanocyte-stimulating hormone receptorHomo sapiens (human)
positive regulation of feeding behaviorMelanocyte-stimulating hormone receptorHomo sapiens (human)
regulation of metabolic processMelanocyte-stimulating hormone receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (8)

Processvia Protein(s)Taxonomy
melanocortin receptor activityMelanocortin receptor 4Homo sapiens (human)
melanocyte-stimulating hormone receptor activityMelanocortin receptor 4Homo sapiens (human)
protein bindingMelanocortin receptor 4Homo sapiens (human)
peptide hormone bindingMelanocortin receptor 4Homo sapiens (human)
ubiquitin protein ligase bindingMelanocortin receptor 4Homo sapiens (human)
neuropeptide bindingMelanocortin receptor 4Homo sapiens (human)
protein bindingMelanocortin receptor 5Homo sapiens (human)
hormone bindingMelanocortin receptor 5Homo sapiens (human)
melanocortin receptor activityMelanocortin receptor 5Homo sapiens (human)
melanocortin receptor activityMelanocortin receptor 3Homo sapiens (human)
melanocyte-stimulating hormone receptor activityMelanocortin receptor 3Homo sapiens (human)
protein bindingMelanocortin receptor 3Homo sapiens (human)
neuropeptide bindingMelanocortin receptor 3Homo sapiens (human)
peptide hormone bindingMelanocortin receptor 3Homo sapiens (human)
melanocortin receptor activityMelanocyte-stimulating hormone receptorHomo sapiens (human)
melanocyte-stimulating hormone receptor activityMelanocyte-stimulating hormone receptorHomo sapiens (human)
protein bindingMelanocyte-stimulating hormone receptorHomo sapiens (human)
G protein-coupled peptide receptor activityMelanocyte-stimulating hormone receptorHomo sapiens (human)
ubiquitin protein ligase bindingMelanocyte-stimulating hormone receptorHomo sapiens (human)
hormone bindingMelanocyte-stimulating hormone receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (3)

Processvia Protein(s)Taxonomy
plasma membraneMelanocortin receptor 4Homo sapiens (human)
membraneMelanocortin receptor 4Homo sapiens (human)
plasma membraneMelanocortin receptor 4Homo sapiens (human)
cytoplasmMelanocortin receptor 4Homo sapiens (human)
plasma membraneMelanocortin receptor 5Homo sapiens (human)
plasma membraneMelanocortin receptor 5Homo sapiens (human)
cytoplasmMelanocortin receptor 5Homo sapiens (human)
plasma membraneMelanocortin receptor 3Homo sapiens (human)
cytoplasmMelanocortin receptor 3Homo sapiens (human)
plasma membraneMelanocortin receptor 3Homo sapiens (human)
plasma membraneMelanocyte-stimulating hormone receptorHomo sapiens (human)
plasma membraneMelanocyte-stimulating hormone receptorHomo sapiens (human)
cytoplasmMelanocyte-stimulating hormone receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (24)

Assay IDTitleYearJournalArticle
AID1852344Selectivity ratio of EC50 for human MC4R to EC50 for human MC1R2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Late-Stage Functionalization with Cysteine Staples Generates Potent and Selective Melanocortin Receptor-1 Agonists.
AID1852338Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Late-Stage Functionalization with Cysteine Staples Generates Potent and Selective Melanocortin Receptor-1 Agonists.
AID1812562Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay2021Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
Melanocortin 1 Receptor Agonists Based on a Bivalent, Bicyclic Peptide Framework.
AID1852339Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Late-Stage Functionalization with Cysteine Staples Generates Potent and Selective Melanocortin Receptor-1 Agonists.
AID1852341Selectivity ratio of Ki for human MC3R to Ki for human MC1R2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Late-Stage Functionalization with Cysteine Staples Generates Potent and Selective Melanocortin Receptor-1 Agonists.
AID1852335Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Late-Stage Functionalization with Cysteine Staples Generates Potent and Selective Melanocortin Receptor-1 Agonists.
AID1852336Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Late-Stage Functionalization with Cysteine Staples Generates Potent and Selective Melanocortin Receptor-1 Agonists.
AID1812563Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay2021Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
Melanocortin 1 Receptor Agonists Based on a Bivalent, Bicyclic Peptide Framework.
AID1812559Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay2021Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
Melanocortin 1 Receptor Agonists Based on a Bivalent, Bicyclic Peptide Framework.
AID1812560Displacement of [125I]-NDP-alpha-MSH from human MC1R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay2021Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
Melanocortin 1 Receptor Agonists Based on a Bivalent, Bicyclic Peptide Framework.
AID1812557Agonist activity at human melanocortin receptor 1 expressed in human T-Rex-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay2021Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
Melanocortin 1 Receptor Agonists Based on a Bivalent, Bicyclic Peptide Framework.
AID1852340Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Late-Stage Functionalization with Cysteine Staples Generates Potent and Selective Melanocortin Receptor-1 Agonists.
AID1852337Agonist activity at human MC1R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Late-Stage Functionalization with Cysteine Staples Generates Potent and Selective Melanocortin Receptor-1 Agonists.
AID1812558Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay2021Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
Melanocortin 1 Receptor Agonists Based on a Bivalent, Bicyclic Peptide Framework.
AID1852334Displacement of [125I]-NDP-alpha-MSH from human MC1R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Late-Stage Functionalization with Cysteine Staples Generates Potent and Selective Melanocortin Receptor-1 Agonists.
AID1812567Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay2021Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
Melanocortin 1 Receptor Agonists Based on a Bivalent, Bicyclic Peptide Framework.
AID1852343Selectivity ratio of EC50 for human MC3R to EC50 for human MC1R2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Late-Stage Functionalization with Cysteine Staples Generates Potent and Selective Melanocortin Receptor-1 Agonists.
AID1812561Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay2021Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
Melanocortin 1 Receptor Agonists Based on a Bivalent, Bicyclic Peptide Framework.
AID1852342Selectivity ratio of Ki for human MC4R to Ki for human MC1R2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Late-Stage Functionalization with Cysteine Staples Generates Potent and Selective Melanocortin Receptor-1 Agonists.
AID1346171Human MC4 receptor (Melanocortin receptors)2009Peptides, Oct, Volume: 30, Issue:10
Analysis of the therapeutic functions of novel melanocortin receptor agonists in MC3R- and MC4R-deficient C57BL/6J mice.
AID1346178Human MC3 receptor (Melanocortin receptors)2009Peptides, Oct, Volume: 30, Issue:10
Analysis of the therapeutic functions of novel melanocortin receptor agonists in MC3R- and MC4R-deficient C57BL/6J mice.
AID1346180Human MC5 receptor (Melanocortin receptors)2009Peptides, Oct, Volume: 30, Issue:10
Analysis of the therapeutic functions of novel melanocortin receptor agonists in MC3R- and MC4R-deficient C57BL/6J mice.
AID1346224Rat MC4 receptor (Melanocortin receptors)2009Peptides, Oct, Volume: 30, Issue:10
Analysis of the therapeutic functions of novel melanocortin receptor agonists in MC3R- and MC4R-deficient C57BL/6J mice.
AID1346231Human MC1 receptor (Melanocortin receptors)2009Peptides, Oct, Volume: 30, Issue:10
Analysis of the therapeutic functions of novel melanocortin receptor agonists in MC3R- and MC4R-deficient C57BL/6J mice.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (39)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's1 (2.56)29.6817
2010's11 (28.21)24.3611
2020's27 (69.23)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 28.05

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 Index28.05 (24.57)
Research Supply Index3.87 (2.92)
Research Growth Index6.13 (4.65)
Search Engine Demand Index31.58 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (28.05)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials8 (20.51%)5.53%
Reviews7 (17.95%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other24 (61.54%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]