Page last updated: 2024-11-12

thapsigargicin

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

Description

thapsigargicin: a hexaoxygenated tetraacylated sesquiterpene lactone tetraester isolated from roots of Thapsia garganica; structure given in first source; it induces mast cell degranulation and histamine release; it (and thapsitranstagin) is an analog of thapsigargin; [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

FloraRankFlora DefinitionFamilyFamily Definition
ThapsiagenusA plant genus of the family APIACEAE. Members contain THAPSIGARGIN and other guaianolides (SESQUITERPENES, GUAIANOLIDE).[MeSH]ApiaceaeA large plant family in the order Apiales, also known as Umbelliferae. Most are aromatic herbs with alternate, feather-divided leaves that are sheathed at the base. The flowers often form a conspicuous flat-topped umbel. Each small individual flower is usually bisexual, with five sepals, five petals, and an enlarged disk at the base of the style. The fruits are ridged and are composed of two parts that split open at maturity.[MeSH]

Cross-References

ID SourceID
PubMed CID10258363
CHEMBL ID328508
MeSH IDM0134273

Synonyms (9)

Synonym
CHEMBL328508
BRD-K73500942-001-01-5
67526-94-7
thapsigargicin
HSCI1_000012
thapsigargicin, >=90%
[(3s,3ar,4s,6s,6ar,7s,8s,9bs)-6-acetyloxy-4-butanoyloxy-3,3a-dihydroxy-3,6,9-trimethyl-8-[(z)-2-methylbut-2-enoyl]oxy-2-oxo-4,5,6a,7,8,9b-hexahydroazuleno[4,5-b]furan-7-yl] hexanoate
HY-N11691
CS-0715246
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (13)

Assay IDTitleYearJournalArticle
AID1395971Inhibition of SERCA in human HeLa cells assessed as increase in cytosolic calcium level at 3.81 x 10'-11M measured over 300 secs by Fluo-4 NW dye based FLIPR analysis relative to control2018Bioorganic & medicinal chemistry letters, 09-01, Volume: 28, Issue:16
Divergent synthesis of thapsigargin analogs.
AID44947Activity against [Ca2+]-ATPase in rabbit myocardial membrane1995Journal of medicinal chemistry, Jan-20, Volume: 38, Issue:2
Structure-activity relationships of analogues of thapsigargin modified at O-11 and O-12.
AID1395969Inhibition of SERCA in human HeLa cells assessed as increase in cytosolic calcium level at 6.10 x 10'-10M measured over 300 secs by Fluo-4 NW dye based FLIPR analysis relative to control2018Bioorganic & medicinal chemistry letters, 09-01, Volume: 28, Issue:16
Divergent synthesis of thapsigargin analogs.
AID242934Inhibitory potency against sarco- endoplasmic reticulum calcium-ATPase in relative to thapsigargin2005Journal of medicinal chemistry, Apr-21, Volume: 48, Issue:8
Applying linear interaction energy method for rational design of noncompetitive allosteric inhibitors of the sarco- and endoplasmic reticulum calcium-ATPase.
AID1395965Inhibition of SERCA in human HeLa cells assessed as increase in cytosolic calcium level at 1.56 x 10'-7M measured over 300 secs by Fluo-4 NW dye based FLIPR analysis relative to control2018Bioorganic & medicinal chemistry letters, 09-01, Volume: 28, Issue:16
Divergent synthesis of thapsigargin analogs.
AID1395962Inhibition of SERCA in human HeLa cells assessed as increase in cytosolic calcium level at 1.00 x 10'-5M measured over 300 secs by Fluo-4 NW dye based FLIPR analysis relative to control2018Bioorganic & medicinal chemistry letters, 09-01, Volume: 28, Issue:16
Divergent synthesis of thapsigargin analogs.
AID1395961Inhibition of SERCA in human HeLa cells assessed as increase in cytosolic calcium level measured over 300 secs by Fluo-4 NW dye based FLIPR analysis2018Bioorganic & medicinal chemistry letters, 09-01, Volume: 28, Issue:16
Divergent synthesis of thapsigargin analogs.
AID1395970Inhibition of SERCA in human HeLa cells assessed as increase in cytosolic calcium level at 1.53 x 10'-10M measured over 300 secs by Fluo-4 NW dye based FLIPR analysis relative to control2018Bioorganic & medicinal chemistry letters, 09-01, Volume: 28, Issue:16
Divergent synthesis of thapsigargin analogs.
AID1395964Inhibition of SERCA in human HeLa cells assessed as increase in cytosolic calcium level at 6.25 x 10'-7M measured over 300 secs by Fluo-4 NW dye based FLIPR analysis relative to control2018Bioorganic & medicinal chemistry letters, 09-01, Volume: 28, Issue:16
Divergent synthesis of thapsigargin analogs.
AID1395966Inhibition of SERCA in human HeLa cells assessed as increase in cytosolic calcium level at 3.91 x 10'-8M measured over 300 secs by Fluo-4 NW dye based FLIPR analysis relative to control2018Bioorganic & medicinal chemistry letters, 09-01, Volume: 28, Issue:16
Divergent synthesis of thapsigargin analogs.
AID1395967Inhibition of SERCA in human HeLa cells assessed as increase in cytosolic calcium level at 9.77 x 10'-9M measured over 300 secs by Fluo-4 NW dye based FLIPR analysis relative to control2018Bioorganic & medicinal chemistry letters, 09-01, Volume: 28, Issue:16
Divergent synthesis of thapsigargin analogs.
AID1395968Inhibition of SERCA in human HeLa cells assessed as increase in cytosolic calcium level at 2.44 x 10'-9M measured over 300 secs by Fluo-4 NW dye based FLIPR analysis relative to control2018Bioorganic & medicinal chemistry letters, 09-01, Volume: 28, Issue:16
Divergent synthesis of thapsigargin analogs.
AID1395963Inhibition of SERCA in human HeLa cells assessed as increase in cytosolic calcium level at 2.50 x 10'-6M measured over 300 secs by Fluo-4 NW dye based FLIPR analysis relative to control2018Bioorganic & medicinal chemistry letters, 09-01, Volume: 28, Issue:16
Divergent synthesis of thapsigargin analogs.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (35)

TimeframeStudies, This Drug (%)All Drugs %
pre-19904 (11.43)18.7374
1990's2 (5.71)18.2507
2000's11 (31.43)29.6817
2010's15 (42.86)24.3611
2020's3 (8.57)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 11.31

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 Index11.31 (24.57)
Research Supply Index3.64 (2.92)
Research Growth Index4.94 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.31)

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%
Other37 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]