Page last updated: 2024-12-10

rn 1734

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

Description

RN 1734: a TRPV4 antagonist; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID3601086
CHEMBL ID2324347
SCHEMBL ID20304906
MeSH IDM0540706

Synonyms (33)

Synonym
2,4-dichloro-n-propan-2-yl-n-[2-(propan-2-ylamino)ethyl]benzenesulfonamide
AKOS005110777
((2,4-dichlorophenyl)sulfonyl)(isopropyl)(2-((isopropyl)amino)ethyl)amine
rn-1734
946387-07-1
2,4-dichloro-n-isopropyl-n-(2-isopropylaminoethyl)benzenesulfonamide
S2650
rn1734
2,4-dichloro-n-(propan-2-yl)-n-{2-[(propan-2-yl)amino]ethyl}benzene-1-sulfonamide
rn 1734
gtpl4294
CHEMBL2324347 ,
bdbm50426575
rn-1734 (2,4-dichloro-n-isopropyl-n-(2-isopropylaminoethyl)benzenesulfonamide)
MS-6135
HB1196
c14h22cl2n2o2s
DTXSID90394046
SCHEMBL20304906
mfcd00129453
CS-5495
HY-19975
rn-1734, >=98% (hplc)
2,4-dichloro-n-isopropyl-n-(2-(isopropylamino)ethyl)benzenesulfonamide
A916431
trpv4 antagonist i, rn-1734 - cas 946387-07-1
HMS3678D05
Q27088563
BCP28123
HMS3414D05
HMS3750M03
trpv4 antagonist i, rn-1734
WMB38707
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (3)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Transient receptor potential cation channel subfamily V member 4 Mus musculus (house mouse)IC50 (µMol)5.90000.01702.95855.9000AID1430785; AID1721331
Transient receptor potential cation channel subfamily V member 4Rattus norvegicus (Norway rat)IC50 (µMol)3.20000.03701.45415.9000AID1430784; AID1721332
Transient receptor potential cation channel subfamily V member 4Homo sapiens (human)IC50 (µMol)2.30000.01802.01349.9000AID1430783; AID1667133; AID1721330; AID726254
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (45)

Processvia Protein(s)Taxonomy
negative regulation of transcription by RNA polymerase IITransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
response to hypoxiaTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
diet induced thermogenesisTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
calcium ion transportTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
intracellular calcium ion homeostasisTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
cell volume homeostasisTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
actin filament organizationTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
cell-cell junction assemblyTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
positive regulation of cytosolic calcium ion concentrationTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
osmosensory signaling pathwayTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
response to mechanical stimulusTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
positive regulation of macrophage chemotaxisTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
negative regulation of neuron projection developmentTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
actin cytoskeleton organizationTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
vasopressin secretionTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
positive regulation of microtubule depolymerizationTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
positive regulation of interleukin-6 productionTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
response to insulinTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
cellular response to heatTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
hyperosmotic salinity responseTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
glucose homeostasisTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
positive regulation of vascular permeabilityTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
cortical microtubule organizationTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
positive regulation of striated muscle contractionTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
positive regulation of JNK cascadeTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
microtubule polymerizationTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
regulation of response to osmotic stressTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
positive regulation of inflammatory responseTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
multicellular organismal-level water homeostasisTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
cartilage development involved in endochondral bone morphogenesisTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
calcium ion importTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
calcium ion transmembrane transportTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
cellular response to osmotic stressTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
cellular hypotonic responseTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
cellular hypotonic salinity responseTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
positive regulation of monocyte chemotactic protein-1 productionTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
positive regulation of macrophage inflammatory protein 1 alpha productionTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
positive regulation of chemokine (C-C motif) ligand 5 productionTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
blood vessel endothelial cell delaminationTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
calcium ion import into cytosolTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
negative regulation of brown fat cell differentiationTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
regulation of aerobic respirationTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
positive regulation of chemokine (C-X-C motif) ligand 1 productionTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
calcium ion import across plasma membraneTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (18)

Processvia Protein(s)Taxonomy
actin bindingTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
osmosensor activityTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
protein kinase C bindingTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
monoatomic cation channel activityTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
calcium channel activityTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
protein bindingTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
calmodulin bindingTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
ATP bindingTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
microtubule bindingTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
lipid bindingTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
stretch-activated, monoatomic cation-selective, calcium channel activityTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
protein kinase bindingTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
SH2 domain bindingTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
identical protein bindingTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
alpha-tubulin bindingTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
metal ion bindingTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
beta-tubulin bindingTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
actin filament bindingTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (14)

Processvia Protein(s)Taxonomy
cytoplasmic microtubuleTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
endoplasmic reticulumTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
plasma membraneTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
adherens junctionTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
focal adhesionTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
ciliumTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
cell surfaceTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
membraneTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
apical plasma membraneTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
lamellipodiumTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
filopodiumTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
growth coneTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
cortical actin cytoskeletonTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
ruffle membraneTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
plasma membraneTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
ciliumTransient receptor potential cation channel subfamily V member 4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (11)

Assay IDTitleYearJournalArticle
AID1430785Antagonist activity at mouse TRPV4 expressed in HEK293 cells assessed as inhibition of 4alpha-PDD-induced intracellular calcium after 10 mins in presence of 45Ca2+ by microbeta liquid scintillation counting method2017ACS medicinal chemistry letters, May-11, Volume: 8, Issue:5
Discovery of GSK2193874: An Orally Active, Potent, and Selective Blocker of Transient Receptor Potential Vanilloid 4.
AID1721330Antagonist activity at human TRPV42020Bioorganic & medicinal chemistry, 08-15, Volume: 28, Issue:16
Modulation of TRPV4 and BKCa for treatment of brain diseases.
AID1430784Antagonist activity at rat TRPV4 expressed in HEK293 cells assessed as inhibition of 4alpha-PDD-induced intracellular calcium after 10 mins in presence of 45Ca2+ by microbeta liquid scintillation counting method2017ACS medicinal chemistry letters, May-11, Volume: 8, Issue:5
Discovery of GSK2193874: An Orally Active, Potent, and Selective Blocker of Transient Receptor Potential Vanilloid 4.
AID726254Inhibition of TRPV4 (unknown origin)2013Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
Ion channels as therapeutic targets: a drug discovery perspective.
AID1721331Antagonist activity at mouse TRPV42020Bioorganic & medicinal chemistry, 08-15, Volume: 28, Issue:16
Modulation of TRPV4 and BKCa for treatment of brain diseases.
AID1721332Antagonist activity at rat TRPV42020Bioorganic & medicinal chemistry, 08-15, Volume: 28, Issue:16
Modulation of TRPV4 and BKCa for treatment of brain diseases.
AID1667133Antagonist activity at TRPV4 (unknown origin)2020Bioorganic & medicinal chemistry letters, 04-15, Volume: 30, Issue:8
Recent advances in TRPV4 agonists and antagonists.
AID1430783Antagonist activity at human TRPV4 expressed in HEK293 cells assessed as inhibition of 4alpha-PDD-induced intracellular calcium after 10 mins in presence of 45Ca2+ by microbeta liquid scintillation counting method2017ACS medicinal chemistry letters, May-11, Volume: 8, Issue:5
Discovery of GSK2193874: An Orally Active, Potent, and Selective Blocker of Transient Receptor Potential Vanilloid 4.
AID1346615Rat TRPV4 (Transient Receptor Potential channels)2009Biochemical and biophysical research communications, Nov-20, Volume: 389, Issue:3
Identification and characterization of novel TRPV4 modulators.
AID1346605Human TRPV4 (Transient Receptor Potential channels)2009Biochemical and biophysical research communications, Nov-20, Volume: 389, Issue:3
Identification and characterization of novel TRPV4 modulators.
AID1346607Mouse TRPV4 (Transient Receptor Potential channels)2009Biochemical and biophysical research communications, Nov-20, Volume: 389, Issue:3
Identification and characterization of novel TRPV4 modulators.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (37)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's1 (2.70)29.6817
2010's32 (86.49)24.3611
2020's4 (10.81)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 29.70

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 Index29.70 (24.57)
Research Supply Index3.66 (2.92)
Research Growth Index6.75 (4.65)
Search Engine Demand Index22.26 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (29.70)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews4 (10.53%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other34 (89.47%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]