Page last updated: 2024-12-08
xv 459
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Market Indicators
Description
XV 459: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 177231 |
| CHEMBL ID | 23743 |
| SCHEMBL ID | 7213400 |
| MeSH ID | M0272444 |
Synonyms (12)
| Synonym |
|---|
| CHEMBL23743 , |
| (2s)-2-(butoxycarbonylamino)-3-[[2-[(5r)-3-(4-carbamimidoylphenyl)-4,5-dihydro-1,2-oxazol-5-yl]acetyl]amino]propanoic acid |
| bdbm50058855 |
| (s)-2-butoxycarbonylamino-3-{2-[(r)-3-(4-carbamimidoyl-phenyl)-4,5-dihydro-isoxazol-5-yl]-acetylamino}-propionic acid; tfa |
| xv 459 |
| l-alanine, 3-(((3-(4-(aminoiminomethyl)phenyl)-4,5-dihydro-5-isoxazolyl)acetyl)amino)-n-(butoxycarbonyl)-, (r)- |
| 170902-52-0 |
| xv459 |
| SCHEMBL7213400 |
| DTXSID80168970 |
| n-(butoxycarbonyl)-3-{2-[(5r)-3-(4-carbamimidoylphenyl)-4,5-dihydro-1,2-oxazol-5-yl]acetamido}-l-alanine |
| AKOS040754476 |
Research Excerpts
Bioavailability
| Excerpt | Reference | Relevance |
|---|---|---|
| "Intranasal absorption and bioavailability of DMP 755, a peptidomimetic, platelet glycoprotein IIb/IIIa receptor antagonist, were examined in anesthetized and lightly sedated dogs." | ( Intranasal absorption of the platelet glycoprotein IIb/IIIa receptor antagonist, DMP 755, and the effect of anesthesia on nasal bioavailability. Aungst, BJ; Hussain, MA; Kapil, R; Mousa, SA, 1997) | 0.3 |
| " DMP754 demonstrated oral bioavailability of 20." | ( Intravenous and oral antithrombotic efficacy of the novel platelet GPIIb/IIIa antagonist roxifiban (DMP754) and its free acid form, XV459. Kapil, R; Mousa, SA; Mu, DX, 1999) | 0.3 |
Dosage Studied
| Excerpt | Relevance | Reference |
|---|---|---|
| " Initial LC/MS identification of metabolites was achieved by dosing the rat with an equimolar mixture of d0:d4 roxifiban and detecting isotopic clusters of pseudomolecular ions." | ( Mass spectrometric and NMR characterization of metabolites of roxifiban, a potent and selective antagonist of the platelet glycoprotein IIb/IIIa receptor. Christ, DD; Diamond, S; Gan, L; Mutlib, AE; Nemeth, G; Shockcor, J; Way, R, 2000) | 0.31 |
| " Measurable plasma concentrations of XV459 appeared rapidly and were sustained throughout the dosing interval of 24 hours." | ( Safety, tolerability, pharmacokinetics, and time course of pharmacologic response of the active metabolite of roxifiban, XV459, a glycoprotein IIb/IIIa antagonist, following oral administration in healthy volunteers. Cain, VA; Ebling, W; Fossler, MJ; Kornhauser, DM; Ma, S; Mondick, JT; Pieniaszek, HJ; Sy, SK, 2002) | 0.31 |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Protein Targets (2)
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Integrin beta-3 | Homo sapiens (human) | IC50 (µMol) | 0.0271 | 0.0001 | 0.6323 | 10.0000 | AID220859; AID221914; AID72989 |
| Integrin alpha-IIb | Homo sapiens (human) | IC50 (µMol) | 0.0271 | 0.0001 | 0.7309 | 10.0000 | AID220859; AID221914; AID72989 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Biological Processes (70)
Molecular Functions (21)
Ceullar Components (30)
Bioassays (6)
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID72989 | Inhibition of fibrinogen (Fg) interaction with GPIIb/IIIa in gel filtered platelets | 1999 | Bioorganic & medicinal chemistry letters, Jan-18, Volume: 9, Issue:2 | Isoxazoline GPIIb/IIIa antagonists bearing a phosphoramidate. |
| AID24314 | biological half-life was measured on unactivated human platelets | 2000 | Journal of medicinal chemistry, Sep-21, Volume: 43, Issue:19 | Platelet glycoprotein IIb-IIIa antagonists as prototypical integrin blockers: novel parenteral and potential oral antithrombotic agents. |
| AID158230 | Inhibition of platelet aggregation in citreated human platelet rich plasma (PRP) | 1999 | Bioorganic & medicinal chemistry letters, Jan-18, Volume: 9, Issue:2 | Isoxazoline GPIIb/IIIa antagonists bearing a phosphoramidate. |
| AID220859 | Affinity for purified human platelet glycoprotein alpha IIb beta3 integrin receptor in ELISA | 1999 | Bioorganic & medicinal chemistry letters, Jan-18, Volume: 9, Issue:2 | Isoxazoline GPIIb/IIIa antagonists bearing a phosphoramidate. |
| AID158231 | Inhibition of platelet aggregation in heparin treated human platelet rich plasma (PRP) | 1999 | Bioorganic & medicinal chemistry letters, Jan-18, Volume: 9, Issue:2 | Isoxazoline GPIIb/IIIa antagonists bearing a phosphoramidate. |
| AID221914 | In vitro inhibition of gel filtered platelet aggregation induced by ADP. | 2000 | Journal of medicinal chemistry, Sep-21, Volume: 43, Issue:19 | Platelet glycoprotein IIb-IIIa antagonists as prototypical integrin blockers: novel parenteral and potential oral antithrombotic agents. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
Research
Studies (15)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 9 (60.00) | 18.2507 |
| 2000's | 6 (40.00) | 29.6817 |
| 2010's | 0 (0.00) | 24.3611 |
| 2020's | 0 (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: 11.33
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.
| This Compound (11.33) All Compounds (24.57) |
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 2 (13.33%) | 5.53% |
| Reviews | 1 (6.67%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 12 (80.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||