Page last updated: 2024-11-12

shu 9119

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

Description

SHU 9119: an agouti mimetic; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID9898183
CHEMBL ID3422426
MeSH IDM0270082

Synonyms (10)

Synonym
(ac-cyclo-[nle4asp5,d-nal(2)7,lys10]alpha-msh-(4-10)-nh2)
gtpl1325
shu 9119
shu-9119
168482-23-3
AKOS024457620
bdbm50080576
CHEMBL3422426 ,
l-lysinamide,n-acetyl-l-norleucyl-l-a-aspartyl-l-histidyl-3-(2-naphthalenyl)-d-alanyl-l-arginyl-l-tryptophyl-,(2(r)7)-lactam
shu9119 (trifluoroacetate salt)

Research Excerpts

Dosage Studied

ExcerptRelevanceReference
" We evaluated the contribution of the caudal brainstem MC system by (1) performing respective dose-response analyses for an MC-R agonist (MTII) and antagonist (SHU9119) delivered to the fourth ventricle, (2) comparing, in the same rats, the fourth intracerebroventricular dose-response profiles to those obtained with lateral intracerebroventricular delivery, and (3) delivering an effective dose of MTII or SHU9119 to rats before a 24 hr period of food deprivation."( Brainstem application of melanocortin receptor ligands produces long-lasting effects on feeding and body weight.
Ginsberg, AB; Grill, HJ; Kaplan, JM; Seeley, RJ, 1998
)
0.3
" Compounds dosed by intracerebroventricular and oral routes reduced PYY-induced food intake and this effect was reversed by the cyclic peptide MC4R antagonist SHU9119."( A concise synthesis of 1,4-dihydro-[1,4]diazepine-5,7-dione, a novel 7-TM receptor ligand core structure with melanocortin receptor agonist activity.
Andrews, JL; Daniels, AJ; Grizzle, MK; Ignar, DM; Laudeman, CP; Minick, DJ; Sammond, DM; Szewczyk, JR; Villeneuve, M, 2010
)
0.36
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (6)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Melanocortin receptor 4Homo sapiens (human)IC50 (µMol)0.03800.00020.64136.1900AID1743771
Melanocortin receptor 4Homo sapiens (human)Ki0.00000.00000.30864.8860AID1743780
Melanocortin receptor 3Homo sapiens (human)IC50 (µMol)0.08310.00120.01660.0832AID1743770
Melanocortin receptor 3Homo sapiens (human)Ki0.00010.00010.24522.8650AID1743779
[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 3Mus musculus (house mouse)EC50 (µMol)0.00300.00010.28575.4000AID1202906
Melanocortin receptor 3Mus musculus (house mouse)Kd0.00120.00030.06730.1995AID1202910; AID1226417
Melanocortin receptor 5Mus musculus (house mouse)EC50 (µMol)0.00240.00000.03211.4900AID1202905; AID1226419
Melanocortin receptor 4Mus musculus (house mouse)EC50 (µMol)100.00000.00000.12472.4700AID1202911
Melanocortin receptor 4Mus musculus (house mouse)Kd0.00010.00000.00180.0050AID1202914; AID1226418
Melanocyte-stimulating hormone receptorMus musculus (house mouse)EC50 (µMol)0.00070.00000.30047.6900AID1202904; AID1226415
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (22)

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)
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)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (6)

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)
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)
[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 3Homo sapiens (human)
cytoplasmMelanocortin receptor 3Homo sapiens (human)
plasma membraneMelanocortin receptor 3Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (26)

Assay IDTitleYearJournalArticle
AID1346178Human MC3 receptor (Melanocortin receptors)2002European journal of pharmacology, Apr-12, Volume: 440, Issue:2-3
The role of melanocortins in body weight regulation: opportunities for the treatment of obesity.
AID1346178Human MC3 receptor (Melanocortin receptors)1999Neuropeptides, Jun, Volume: 33, Issue:3
Further pharmacological characterization of the selective melanocortin 4 receptor antagonist HS014: comparison with SHU9119.
AID1346171Human MC4 receptor (Melanocortin receptors)1999European journal of pharmacology, Aug-13, Volume: 378, Issue:3
Characterization of melanocortin receptor ligands on cloned brain melanocortin receptors and on grooming behavior in the rat.
AID1346180Human MC5 receptor (Melanocortin receptors)1999Neuropeptides, Jun, Volume: 33, Issue:3
Further pharmacological characterization of the selective melanocortin 4 receptor antagonist HS014: comparison with SHU9119.
AID1346179Rat MC3 receptor (Melanocortin receptors)1999European journal of pharmacology, Aug-13, Volume: 378, Issue:3
Characterization of melanocortin receptor ligands on cloned brain melanocortin receptors and on grooming behavior in the rat.
AID1346231Human MC1 receptor (Melanocortin receptors)1995Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18
Cyclic lactam alpha-melanotropin analogues of Ac-Nle4-cyclo[Asp5, D-Phe7,Lys10] alpha-melanocyte-stimulating hormone-(4-10)-NH2 with bulky aromatic amino acids at position 7 show high antagonist potency and selectivity at specific melanocortin receptors.
AID1346178Human MC3 receptor (Melanocortin receptors)1995Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18
Cyclic lactam alpha-melanotropin analogues of Ac-Nle4-cyclo[Asp5, D-Phe7,Lys10] alpha-melanocyte-stimulating hormone-(4-10)-NH2 with bulky aromatic amino acids at position 7 show high antagonist potency and selectivity at specific melanocortin receptors.
AID1346231Human MC1 receptor (Melanocortin receptors)1999Neuropeptides, Jun, Volume: 33, Issue:3
Further pharmacological characterization of the selective melanocortin 4 receptor antagonist HS014: comparison with SHU9119.
AID1346171Human MC4 receptor (Melanocortin receptors)1999Neuropeptides, Jun, Volume: 33, Issue:3
Further pharmacological characterization of the selective melanocortin 4 receptor antagonist HS014: comparison with SHU9119.
AID1743779Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins2021Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
Structure-Based Design of Melanocortin 4 Receptor Ligands Based on the SHU-9119-hMC4R Cocrystal Structure†.
AID1743780Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins2021Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
Structure-Based Design of Melanocortin 4 Receptor Ligands Based on the SHU-9119-hMC4R Cocrystal Structure†.
AID1743772Selectivity index, ratio of IC50 for antagonist activity at human MC4R expressed in HEK293 cells to IC50 for antagonist activity at human MC3R expressed in HEK293 cells2021Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
Structure-Based Design of Melanocortin 4 Receptor Ligands Based on the SHU-9119-hMC4R Cocrystal Structure†.
AID1226415Agonist activity at mouse MC1R expressed in HEK293 cells by cAMP functional bioassay2015Journal of medicinal chemistry, Jun-11, Volume: 58, Issue:11
Discovery of a β-Hairpin Octapeptide, c[Pro-Arg-Phe-Phe-Dap-Ala-Phe-DPro], Mimetic of Agouti-Related Protein(87-132) [AGRP(87-132)] with Equipotent Mouse Melanocortin-4 Receptor (mMC4R) Antagonist Pharmacology.
AID1202906Agonist activity at mouse melanocortin-3 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay2015ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
Melanocortin antagonist tetrapeptides with minimal agonist activity at the mouse melanocortin-3 receptor.
AID1226419Agonist activity at mouse MC5R expressed in HEK293 cells by cAMP functional bioassay2015Journal of medicinal chemistry, Jun-11, Volume: 58, Issue:11
Discovery of a β-Hairpin Octapeptide, c[Pro-Arg-Phe-Phe-Dap-Ala-Phe-DPro], Mimetic of Agouti-Related Protein(87-132) [AGRP(87-132)] with Equipotent Mouse Melanocortin-4 Receptor (mMC4R) Antagonist Pharmacology.
AID1743770Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay2021Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
Structure-Based Design of Melanocortin 4 Receptor Ligands Based on the SHU-9119-hMC4R Cocrystal Structure†.
AID1202905Agonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay2015ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
Melanocortin antagonist tetrapeptides with minimal agonist activity at the mouse melanocortin-3 receptor.
AID1743781Selectivity index, ratio of Ki for human MC3R expressed in HEK293 cell membranes to Ki for human MC4R expressed in HEK293 cell membranes2021Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
Structure-Based Design of Melanocortin 4 Receptor Ligands Based on the SHU-9119-hMC4R Cocrystal Structure†.
AID1202911Agonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay2015ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
Melanocortin antagonist tetrapeptides with minimal agonist activity at the mouse melanocortin-3 receptor.
AID1202910Competitive antagonist activity at mouse melanocortin-3 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysis2015ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
Melanocortin antagonist tetrapeptides with minimal agonist activity at the mouse melanocortin-3 receptor.
AID1743771Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay2021Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
Structure-Based Design of Melanocortin 4 Receptor Ligands Based on the SHU-9119-hMC4R Cocrystal Structure†.
AID1202914Competitive antagonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysis2015ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
Melanocortin antagonist tetrapeptides with minimal agonist activity at the mouse melanocortin-3 receptor.
AID1226417Displacement of MTII from mouse MC3R expressed in HEK293 cells2015Journal of medicinal chemistry, Jun-11, Volume: 58, Issue:11
Discovery of a β-Hairpin Octapeptide, c[Pro-Arg-Phe-Phe-Dap-Ala-Phe-DPro], Mimetic of Agouti-Related Protein(87-132) [AGRP(87-132)] with Equipotent Mouse Melanocortin-4 Receptor (mMC4R) Antagonist Pharmacology.
AID1202907Agonist activity at mouse melanocortin-3 receptor transfected in HEK293 cells at 1 uM after 6 hrs by beta-galactosidase reporter gene assay relative to MTII-induced maximal response2015ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
Melanocortin antagonist tetrapeptides with minimal agonist activity at the mouse melanocortin-3 receptor.
AID1226418Displacement of MTII from mouse MC4R expressed in HEK293 cells2015Journal of medicinal chemistry, Jun-11, Volume: 58, Issue:11
Discovery of a β-Hairpin Octapeptide, c[Pro-Arg-Phe-Phe-Dap-Ala-Phe-DPro], Mimetic of Agouti-Related Protein(87-132) [AGRP(87-132)] with Equipotent Mouse Melanocortin-4 Receptor (mMC4R) Antagonist Pharmacology.
AID1202904Agonist activity at mouse melanocortin-1 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay2015ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
Melanocortin antagonist tetrapeptides with minimal agonist activity at the mouse melanocortin-3 receptor.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (195)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's19 (9.74)18.2507
2000's99 (50.77)29.6817
2010's70 (35.90)24.3611
2020's7 (3.59)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 22.85

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 Index22.85 (24.57)
Research Supply Index5.29 (2.92)
Research Growth Index4.81 (4.65)
Search Engine Demand Index26.67 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (22.85)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (0.51%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other197 (99.49%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]