Page last updated: 2024-12-11
bimosiamose
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Market Indicators
Description
bimosiamose: a selectin inhibitor [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 9811353 |
| CHEMBL ID | 1215923 |
| SCHEMBL ID | 12182030 |
| MeSH ID | M0481217 |
Synonyms (33)
| Synonym |
|---|
| CHEMBL1215923 , |
| tbc 1269 |
| (1,1'-biphenyl)-3-acetic acid, 3',3'''-(1,6-hexanediyl)bis(6'-(alpha-d-mannopyranosyloxy)- |
| bimosiamose |
| (hexane-1,6-diylbis(6'-(alpha-d-mannopyranosyloxy)biphenyl-3',3-diyl))diacetic acid |
| tbc-1269 |
| NCGC00183833-01 |
| bimosiamose [inn] |
| 1,6-bis(3-(3-carboxymethylphenyl)-4-(2-alpha-d-mannopyranosyloxy)phenyl)hexane |
| 97b5kcw80w , |
| 187269-40-5 |
| unii-97b5kcw80w |
| dtxsid8048783 , |
| cas-187269-40-5 |
| dtxcid4028709 |
| tox21_113260 |
| SCHEMBL12182030 |
| 1,6-bis[3-(3-carboxymethylphenyl)-4-(2-r-d-mannopyranosyloxy)phenyl]hexane |
| bdbm50324667 |
| bimosiamose [mi] |
| (hexane-1,6-diylbis(6'-(.alpha.-d-mannopyranosyloxy)biphenyl-3',3-diyl))diacetic acid |
| bimo |
| 2-[3-[5-[6-[3-[3-(carboxymethyl)phenyl]-4-[(2r,3s,4s,5s,6r)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxyphenyl]hexyl]-2-[(2r,3s,4s,5s,6r)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxyphenyl]phenyl]acetic acid |
| compound 15e [pmid: 9544210] |
| gtpl9049 |
| tbc1269 |
| HY-106139 |
| CS-0024963 |
| DB06197 |
| Q27075271 |
| MS-31594 |
| 2,2'-(hexane-1,6-diylbis(6'-(((2r,3s,4s,5s,6r)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2h-pyran-2-yl)oxy)-[1,1'-biphenyl]-3',3-diyl))diacetic acid |
| AKOS040741338 |
Research Excerpts
Overview
Bimosiamose is a novel synthetic panselectin antagonist being developed for the treatment of acute and chronic inflammatory disorders.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Bimosiamose is a novel synthetic panselectin antagonist being developed for the treatment of acute and chronic inflammatory disorders. " | ( Physiochemical properties, safety and pharmacokinetics of bimosiamose disodium after intravenous administration. Jilma, B; Meyer, M; Wolff, G; Zahlten, R, 2005) | 2.02 |
| "Bimosiamose is a novel synthetic pan-selectin antagonist developed for the treatment of acute and chronic inflammatory disorders. " | ( The pharmacokinetics of subcutaneously injected Bimosiamose disodium in healthy male volunteers. Beyer, D; Jilma, B; Meyer, M; Vollhardt, K; Woischwill, C; Wolff, G, 2007) | 2.04 |
Treatment
| Excerpt | Reference | Relevance |
|---|---|---|
| "Treatment with bimosiamose had no significant effect on LPS-induced TF expression, as quantified by TF mRNA levels, or on LPS-induced coagulation response, reflected by increases in plasma thrombin-antithrombin (TAT) complexes and prothrombin fragment (F1 + 2) levels." | ( Effects of the pan-selectin antagonist bimosiamose (TBC1269) in experimental human endotoxemia. Beyer, D; Firbas, C; Jilma, B; Leitner, JM; Mayr, FB; Meyer, M; Reiter, RA; Spiel, AO; Wolff, G, 2008) | 0.95 |
Toxicity
| Excerpt | Reference | Relevance |
|---|---|---|
| " Bimosiamose was safe and well-tolerated." | ( Physiochemical properties, safety and pharmacokinetics of bimosiamose disodium after intravenous administration. Jilma, B; Meyer, M; Wolff, G; Zahlten, R, 2005) | 1.48 |
Pharmacokinetics
| Excerpt | Reference | Relevance |
|---|---|---|
| " This resulted in discovery of PSI-421 with marked improvement in aqueous solubility and pharmacokinetic properties." | ( Discovery of 2-[1-(4-chlorophenyl)cyclopropyl]-3-hydroxy-8-(trifluoromethyl)quinoline-4-carboxylic acid (PSI-421), a P-selectin inhibitor with improved pharmacokinetic properties and oral efficacy in models of vascular injury. Bedard, PW; Clerin, V; Di, L; Huang, A; Janz, K; Kaila, N; Keith, JC; Lowe, M; Moretto, A; Schaub, RG; Shaw, GD; Sushkova, N; Tam, S; Tchernychev, B; Tsao, DH; Wang, Q, 2010) | 0.36 |
Bioavailability
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Protein Targets (7)
Potency Measurements
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Luciferase | Photinus pyralis (common eastern firefly) | Potency | 40.5334 | 0.0072 | 15.7588 | 89.3584 | AID624030 |
| GLI family zinc finger 3 | Homo sapiens (human) | Potency | 0.0030 | 0.0007 | 14.5928 | 83.7951 | AID1259369 |
| AR protein | Homo sapiens (human) | Potency | 26.8325 | 0.0002 | 21.2231 | 8,912.5098 | AID743063 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| P-selectin | Homo sapiens (human) | IC50 (µMol) | 82.5000 | 5.0000 | 5.0000 | 5.0000 | AID280291; AID499878 |
| E-selectin | Homo sapiens (human) | IC50 (µMol) | 500.0000 | 0.0200 | 2.2133 | 6.6000 | AID280289 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Biological Processes (27)
Molecular Functions (17)
Ceullar Components (14)
Bioassays (44)
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID275268 | Inhibition of P-selectin-mediated adhesion of HL60 cells | 2007 | Journal of medicinal chemistry, Jan-11, Volume: 50, Issue:1 | Synthesis and biological evaluation of quinoline salicylic acids as P-selectin antagonists. |
| AID280293 | Inhibition of human L-selectin after 2 hrs | 2007 | Journal of medicinal chemistry, Mar-22, Volume: 50, Issue:6 | Rational design of novel, potent small molecule pan-selectin antagonists. |
| AID499878 | Inhibition of P-selectin in human HL-60 cells | 2010 | Journal of medicinal chemistry, Aug-26, Volume: 53, Issue:16 | Discovery of 2-[1-(4-chlorophenyl)cyclopropyl]-3-hydroxy-8-(trifluoromethyl)quinoline-4-carboxylic acid (PSI-421), a P-selectin inhibitor with improved pharmacokinetic properties and oral efficacy in models of vascular injury. |
| AID275270 | Effect on antigen-induced airway hyperresponsiveness in allergic sheep at 10 mg aerosol | 2007 | Journal of medicinal chemistry, Jan-11, Volume: 50, Issue:1 | Synthesis and biological evaluation of quinoline salicylic acids as P-selectin antagonists. |
| AID280296 | Inhibition of attachment of HL60 cells to P-selectin at 109 uM after 5 mins | 2007 | Journal of medicinal chemistry, Mar-22, Volume: 50, Issue:6 | Rational design of novel, potent small molecule pan-selectin antagonists. |
| AID280289 | Inhibition of human E-selectin after 2 hrs | 2007 | Journal of medicinal chemistry, Mar-22, Volume: 50, Issue:6 | Rational design of novel, potent small molecule pan-selectin antagonists. |
| AID280291 | Inhibition of human P-selectin after 2 hrs | 2007 | Journal of medicinal chemistry, Mar-22, Volume: 50, Issue:6 | Rational design of novel, potent small molecule pan-selectin antagonists. |
| AID280295 | Inhibition of attachment of HL60 cells to E-selectin at 109 uM after 5 mins | 2007 | Journal of medicinal chemistry, Mar-22, Volume: 50, Issue:6 | Rational design of novel, potent small molecule pan-selectin antagonists. |
| AID275269 | Effect on survival of kidney allograft in ACI rat at 10 mg/kg, iv | 2007 | Journal of medicinal chemistry, Jan-11, Volume: 50, Issue:1 | Synthesis and biological evaluation of quinoline salicylic acids as P-selectin antagonists. |
| AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
| AID1347097 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347154 | Primary screen GU AMC qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347424 | RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The Journal of biological chemistry, 11-15, Volume: 294, Issue:46 | Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens. |
| AID1347099 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347101 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347103 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347083 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1508630 | Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
| AID1347086 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347092 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347091 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| AID1347425 | Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The Journal of biological chemistry, 11-15, Volume: 294, Issue:46 | Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens. |
| AID1347082 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347107 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347104 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347105 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347093 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347090 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347094 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347108 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347096 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347100 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347106 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347089 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1347102 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347407 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| AID1347095 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347098 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
Research
Studies (25)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 10 (40.00) | 29.6817 |
| 2010's | 9 (36.00) | 24.3611 |
| 2020's | 6 (24.00) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
Market Indicators
Research Demand Index: 20.29
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.
| This Compound (20.29) All Compounds (24.57) |
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 8 (32.00%) | 5.53% |
| Reviews | 2 (8.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 15 (60.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||