Page last updated: 2024-11-07

cgs 22652

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

Description

CGS 22652: has thromboxane receptor antagonism combined with thromboxane synthase inhibition; structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID131717
CHEMBL ID65414
SCHEMBL ID9710116
MeSH IDM0209874

Synonyms (21)

Synonym
3-pyridineheptanoic acid, gamma-(4-(((4-chlorophenyl)sulfonyl)amino)butyl)-, (+-)-
(r,s)-8-((4-chlorophenylsulfonyl)amino)-4-(3-(3-pyridinyl)propyl)octanoic acid
cgs 22652
cgs-22652
(+-)-gamma-(4-(((4-chlorophenyl)sulfonyl)amino)butyl)-3-pyridineheptanoic acid
CHEMBL65414 ,
L004635
8-(4-chloro-benzenesulfonylamino)-4-(3-pyridin-3-yl-propyl)-octanoic acid
bdbm50003776
8-[(4-chlorophenyl)sulfonylamino]-4-(3-pyridin-3-ylpropyl)octanoic acid
unii-30va6wh2e7
30va6wh2e7 ,
134235-78-2
8-(p-chlorophenylsulfonamido)-4-[3-(3-pyridyl)propyl]-octanoic acid
ISMHAZMNDUAHLK-UHFFFAOYSA-N
8-(p-chlorophenylsulfonamido)4-[3-(3-pyridyl)-propyl]-octanoic acid
SCHEMBL9710116
3-pyridineheptanoic acid, .gamma.-(4-(((4-chlorophenyl)sulfonyl)amino)butyl)-, (+/-)-
8-(4-chlorophenylsulfonamido)-4-(3-(pyridin-3-yl)propyl)octanoic acid
DTXSID30928526
8-[(4-chlorobenzene-1-sulfonyl)amino]-4-[3-(pyridin-3-yl)propyl]octanoic acid

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
" The good bioavailability and the long duration of action of some of these compounds was demonstrated using ex vivo measurement of the TxRA activity upon oral administration to guinea pigs."( Thromboxane receptor antagonism combined with thromboxane synthase inhibition. 4. 8-[[(4-Chlorophenyl)sulfonyl]amino]-4-(3-(3-pyridinyl) propyl)octanoic acid and analogs.
Bhagwat, SS; Boswell, C; Cohen, DS; Contardo, N; Dotson, R; Furness, P; Gude, C; Lee, W; Mathis, J; Zoganas, H, 1992
)
0.28
" This indicates that the enantiomers have pharmacologic profile and bioavailability similar to that of the corresponding racemic compound."( Thromboxane receptor antagonism combined with thromboxane synthase inhibition. 5. Synthesis and evaluation of enantiomers of 8-[[(4-chlorophenyl)sulfonyl]amino]-4-(3-pyridinylalkyl)octanoic acid.
Bhagwat, SS; Cohen, DS; Dotson, R; Furness, P; Gude, C; Lee, W; Mathis, J, 1993
)
0.29
[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)
Thromboxane A2 receptor Homo sapiens (human)IC50 (µMol)0.00600.00110.71065.2000AID212272
Thromboxane-A synthase Homo sapiens (human)IC50 (µMol)0.00600.00091.230410.0000AID212099; AID212606; AID212628; AID215775
Thromboxane-A synthaseRattus norvegicus (Norway rat)IC50 (µMol)0.00500.00400.39231.5000AID212099
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (22)

Processvia Protein(s)Taxonomy
smooth muscle contractionThromboxane A2 receptor Homo sapiens (human)
G protein-coupled receptor signaling pathwayThromboxane A2 receptor Homo sapiens (human)
response to nutrientThromboxane A2 receptor Homo sapiens (human)
response to xenobiotic stimulusThromboxane A2 receptor Homo sapiens (human)
positive regulation of blood coagulationThromboxane A2 receptor Homo sapiens (human)
response to testosteroneThromboxane A2 receptor Homo sapiens (human)
thromboxane A2 signaling pathwayThromboxane A2 receptor Homo sapiens (human)
response to ethanolThromboxane A2 receptor Homo sapiens (human)
positive regulation of angiogenesisThromboxane A2 receptor Homo sapiens (human)
positive regulation of smooth muscle contractionThromboxane A2 receptor Homo sapiens (human)
cellular response to lipopolysaccharideThromboxane A2 receptor Homo sapiens (human)
negative regulation of cell migration involved in sprouting angiogenesisThromboxane A2 receptor Homo sapiens (human)
inflammatory responseThromboxane A2 receptor Homo sapiens (human)
positive regulation of blood pressureThromboxane A2 receptor Homo sapiens (human)
positive regulation of vasoconstrictionThromboxane A2 receptor Homo sapiens (human)
positive regulation of cytosolic calcium ion concentrationThromboxane A2 receptor Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayThromboxane A2 receptor Homo sapiens (human)
prostaglandin biosynthetic processThromboxane-A synthase Homo sapiens (human)
icosanoid metabolic processThromboxane-A synthase Homo sapiens (human)
cyclooxygenase pathwayThromboxane-A synthase Homo sapiens (human)
intracellular chloride ion homeostasisThromboxane-A synthase Homo sapiens (human)
response to ethanolThromboxane-A synthase Homo sapiens (human)
positive regulation of vasoconstrictionThromboxane-A synthase Homo sapiens (human)
response to fatty acidThromboxane-A synthase Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (10)

Processvia Protein(s)Taxonomy
thromboxane A2 receptor activityThromboxane A2 receptor Homo sapiens (human)
guanyl-nucleotide exchange factor activityThromboxane A2 receptor Homo sapiens (human)
protein bindingThromboxane A2 receptor Homo sapiens (human)
monooxygenase activityThromboxane-A synthase Homo sapiens (human)
thromboxane-A synthase activityThromboxane-A synthase Homo sapiens (human)
iron ion bindingThromboxane-A synthase Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygenThromboxane-A synthase Homo sapiens (human)
heme bindingThromboxane-A synthase Homo sapiens (human)
12-hydroxyheptadecatrienoic acid synthase activityThromboxane-A synthase Homo sapiens (human)
hydroperoxy icosatetraenoate dehydratase activityThromboxane-A synthase Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (6)

Processvia Protein(s)Taxonomy
acrosomal vesicleThromboxane A2 receptor Homo sapiens (human)
plasma membraneThromboxane A2 receptor Homo sapiens (human)
nuclear speckThromboxane A2 receptor Homo sapiens (human)
plasma membraneThromboxane A2 receptor Homo sapiens (human)
endoplasmic reticulumThromboxane-A synthase Homo sapiens (human)
endoplasmic reticulum membraneThromboxane-A synthase Homo sapiens (human)
cytosolThromboxane-A synthase Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (18)

Assay IDTitleYearJournalArticle
AID223070Inhibition of U 46619-induced Aggregation of human Washed platelets1993Journal of medicinal chemistry, Jan-22, Volume: 36, Issue:2
Thromboxane receptor antagonism combined with thromboxane synthase inhibition. 5. Synthesis and evaluation of enantiomers of 8-[[(4-chlorophenyl)sulfonyl]amino]-4-(3-pyridinylalkyl)octanoic acid.
AID212099Inhibition test of thromboxane A2 synthetase in human gel-filtered platelets.1994Journal of medicinal chemistry, Jan-07, Volume: 37, Issue:1
6,6-Disubstituted Hex-5-enoic acid derivatives as combined thromboxane A2 receptor antagonists and synthetase inhibitors.
AID212272Displacement of the high affinity radiolabeled ligand [3H]- SQ-29548 from the PGH-2/TXA-2 receptor in human gel-filtered platelets.1994Journal of medicinal chemistry, Jan-07, Volume: 37, Issue:1
6,6-Disubstituted Hex-5-enoic acid derivatives as combined thromboxane A2 receptor antagonists and synthetase inhibitors.
AID158082Inhibition of collagen-induced platelet aggregation in human platelet-rich plasma.1994Journal of medicinal chemistry, Jan-07, Volume: 37, Issue:1
6,6-Disubstituted Hex-5-enoic acid derivatives as combined thromboxane A2 receptor antagonists and synthetase inhibitors.
AID77240Inhibition of bronchoconstriction in guinea pigs1992Journal of medicinal chemistry, Nov-13, Volume: 35, Issue:23
Thromboxane receptor antagonism combined with thromboxane synthase inhibition. 4. 8-[[(4-Chlorophenyl)sulfonyl]amino]-4-(3-(3-pyridinyl) propyl)octanoic acid and analogs.
AID80178Ex vivo inhibition of U-46,619-induced aggregation of guinea pig platelets after peroral administration of 10 mg/kg dose at 6 hr time1992Journal of medicinal chemistry, Nov-13, Volume: 35, Issue:23
Thromboxane receptor antagonism combined with thromboxane synthase inhibition. 4. 8-[[(4-Chlorophenyl)sulfonyl]amino]-4-(3-(3-pyridinyl) propyl)octanoic acid and analogs.
AID80175Ex vivo Inhibition of U 46619-induced aggregation of guinea pig platelets at the dose of 10 mg/Kg po per hour expressed as concentration ratio (EC50 of drug/EC50 of control)1993Journal of medicinal chemistry, Jan-22, Volume: 36, Issue:2
Thromboxane receptor antagonism combined with thromboxane synthase inhibition. 5. Synthesis and evaluation of enantiomers of 8-[[(4-chlorophenyl)sulfonyl]amino]-4-(3-pyridinylalkyl)octanoic acid.
AID215775In vitro inhibition of thromboxane synthetase in microsomal platelet preparation1993Journal of medicinal chemistry, Jan-22, Volume: 36, Issue:2
Thromboxane receptor antagonism combined with thromboxane synthase inhibition. 5. Synthesis and evaluation of enantiomers of 8-[[(4-chlorophenyl)sulfonyl]amino]-4-(3-pyridinylalkyl)octanoic acid.
AID159931In vitro inhibition of U 46619 induced aggregation of washed platelets1992Journal of medicinal chemistry, Nov-13, Volume: 35, Issue:23
Thromboxane receptor antagonism combined with thromboxane synthase inhibition. 4. 8-[[(4-Chlorophenyl)sulfonyl]amino]-4-(3-(3-pyridinyl) propyl)octanoic acid and analogs.
AID62836The compound was tested in vitro for its inhibitory activity against U 46619-induced contraction of saphenous vein in dog.1992Journal of medicinal chemistry, Nov-13, Volume: 35, Issue:23
Thromboxane receptor antagonism combined with thromboxane synthase inhibition. 3. Pyridinylalkyl-substituted 8-[(arylsulfonyl)amino]octanoic acids.
AID222770Inhibition of U 46619-induced Aggregation of Human Platelet-rich Plasma1993Journal of medicinal chemistry, Jan-22, Volume: 36, Issue:2
Thromboxane receptor antagonism combined with thromboxane synthase inhibition. 5. Synthesis and evaluation of enantiomers of 8-[[(4-chlorophenyl)sulfonyl]amino]-4-(3-pyridinylalkyl)octanoic acid.
AID60981Evaluated for contraction of dog saphenous vein1992Journal of medicinal chemistry, Nov-13, Volume: 35, Issue:23
Thromboxane receptor antagonism combined with thromboxane synthase inhibition. 4. 8-[[(4-Chlorophenyl)sulfonyl]amino]-4-(3-(3-pyridinyl) propyl)octanoic acid and analogs.
AID212606In vitro inhibition of Thromboxane A2 synthase1992Journal of medicinal chemistry, Nov-13, Volume: 35, Issue:23
Thromboxane receptor antagonism combined with thromboxane synthase inhibition. 4. 8-[[(4-Chlorophenyl)sulfonyl]amino]-4-(3-(3-pyridinyl) propyl)octanoic acid and analogs.
AID92518The compound was tested in vitro for its inhibitory activity against U 46619-induced aggregation of human platelet rich plasma (PRP).1992Journal of medicinal chemistry, Nov-13, Volume: 35, Issue:23
Thromboxane receptor antagonism combined with thromboxane synthase inhibition. 3. Pyridinylalkyl-substituted 8-[(arylsulfonyl)amino]octanoic acids.
AID93152The compound was tested in vitro for its inhibitory activity against U 46619-induced aggregation of washed human platelets.1992Journal of medicinal chemistry, Nov-13, Volume: 35, Issue:23
Thromboxane receptor antagonism combined with thromboxane synthase inhibition. 3. Pyridinylalkyl-substituted 8-[(arylsulfonyl)amino]octanoic acids.
AID212628The compound was tested in vitro for its inhibitory activity against thromboxane synthase A2 (TXA2)1992Journal of medicinal chemistry, Nov-13, Volume: 35, Issue:23
Thromboxane receptor antagonism combined with thromboxane synthase inhibition. 3. Pyridinylalkyl-substituted 8-[(arylsulfonyl)amino]octanoic acids.
AID80177Ex vivo inhibition of U-46,619-induced aggregation of guinea pig platelets after peroral administration of 10 mg/kg dose at 1 hr time1992Journal of medicinal chemistry, Nov-13, Volume: 35, Issue:23
Thromboxane receptor antagonism combined with thromboxane synthase inhibition. 4. 8-[[(4-Chlorophenyl)sulfonyl]amino]-4-(3-(3-pyridinyl) propyl)octanoic acid and analogs.
AID159930Evaluated in vitro for the inhibition of U 46619 induced aggregation of platelet-rich plasma1992Journal of medicinal chemistry, Nov-13, Volume: 35, Issue:23
Thromboxane receptor antagonism combined with thromboxane synthase inhibition. 4. 8-[[(4-Chlorophenyl)sulfonyl]amino]-4-(3-(3-pyridinyl) propyl)octanoic acid and analogs.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (9)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's9 (100.00)18.2507
2000's0 (0.00)29.6817
2010's0 (0.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.05

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 weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index12.05 (24.57)
Research Supply Index2.40 (2.92)
Research Growth Index4.45 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.05)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other10 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]