Page last updated: 2024-12-11
denufosol tetrasodium
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Market Indicators
Description
denufosol tetrasodium: for treatment of cystic fibrosis [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 10219163 |
| CHEMBL ID | 1767407 |
| MeSH ID | M0438654 |
| PubMed CID | 9875516 |
| CHEMBL ID | 507282 |
| SCHEMBL ID | 24414847 |
| MeSH ID | M0438654 |
Synonyms (45)
| Synonym |
|---|
| uridine 5'-(pentahydrogen tetraphosphate), p'''-5'-ester with 2'-deoxycytidine, tetrasodium salt |
| denufosol tetrasodium salt |
| 318250-11-2 |
| denufosol tetrasodium (usan) |
| D03685 |
| denufosol tetrasodium |
| ins-37217 |
| ins37217 |
| ins 37217 |
| chembl1767407 , |
| 82m942wz4a , |
| 2'-deoxycytidine(5')tetraphospho(5')uridine tetrasodium salt |
| uridine 5'-(pentahydrogen tetraphosphate), p'''-5'-ester with ''-deoxycytidine, tetrasodium salt |
| denufosol tetrasodium [usan] |
| unii-82m942wz4a |
| uridine 5'-(pentahydrogen tetraphosphate), p'''->5'-ester with ''-deoxycytidine, tetrasodium salt |
| denufosol tetrasodium salt [mi] |
| denufosol tetrasodium [mart.] |
| HY-U00196 |
| CS-7295 |
| uridine 5'-(pentahydrogen tetraphosphate), 2'-deoxy-, p''' inverted exclamation marku5'-ester with cytidine, tetrasodium salt |
| tetrasodium;[[(2r,3s,5r)-5-(4-amino-2-oxopyrimidin-1-yl)-3-hydroxyoxolan-2-yl]methoxy-oxidophosphoryl] [[[(2r,3s,4r,5r)-5-(2,4-dioxopyrimidin-1-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-oxidophosphoryl]oxy-oxidophosphoryl] phosphate |
| Q27269345 |
| 318250-11-2 (sodium) |
| [[[[(2r,3s,5r)-5-(4-amino-2-oxopyrimidin-1-yl)-3-hydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-hydroxyphosphoryl]oxy-hydroxyphosphoryl] [(2r,3s,4r,5r)-5-(2,4-dioxopyrimidin-1-yl)-3,4-dihydroxyoxolan-2-yl]methyl hydrogen phosphate |
| gtpl1737 |
| up4dc |
| dcp4u |
| bdbm50270553 |
| denufosol |
| CHEMBL507282 , |
| ins 3721 |
| p(1)-(uridine 5')-p(4)-(2'-deoxycytidine 5')tetraphosphate, tetrasodium salt |
| unii-5pc250kssh |
| 5pc250kssh , |
| denufosol [inn] |
| 211448-85-0 |
| ins3721 |
| denufosol [mi] |
| denufosol [who-dd] |
| DB04983 |
| Q908026 |
| uridine 5'-(pentahydrogen tetraphosphate), 2'-deoxy-, p''' inverted exclamation marku5'-ester with cytidine |
| DTXSID50870235 |
| SCHEMBL24414847 |
Research Excerpts
Toxicity
Dosage Studied
| Excerpt | Relevance | Reference |
|---|---|---|
| " Forced expiratory volume in 1 sec (FEV(1)) profiles following dosing were similar across treatment groups, with some acute, reversible decline seen in both groups, most notably in subjects with lower lung function at baseline." | ( Safety and tolerability of denufosol tetrasodium inhalation solution, a novel P2Y2 receptor agonist: results of a phase 1/phase 2 multicenter study in mild to moderate cystic fibrosis. Daines, C; Deterding, R; Engels, J; Gibson, R; Gorden, J; Lavange, L; Marshall, B; Mathews, D; Milgram, L; Milla, C; Ramsey, B; Retsch-Bogart, G; Schaberg, A; Williams, J; Zeitlin, PL, 2005) | 0.33 |
| " All treatments were generally well tolerated, with no dose-response trends observed with respect to safety parameters." | ( Phase 2 randomized safety and efficacy trial of nebulized denufosol tetrasodium in cystic fibrosis. Brody, AS; Coquillette, SJ; Deterding, RR; Engels, JM; Lavange, LM; Mathews, DW; Millard, SP; Ramsey, BW, 2007) | 0.34 |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Protein Targets (3)
Activation Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| P2Y purinoceptor 2 | Homo sapiens (human) | EC50 (µMol) | 0.2000 | 0.0056 | 0.6828 | 10.0000 | AID593134 |
| P2Y purinoceptor 4 | Homo sapiens (human) | EC50 (µMol) | 0.8000 | 0.0230 | 1.3623 | 10.0000 | AID593135 |
| P2Y purinoceptor 6 | Homo sapiens (human) | EC50 (µMol) | 1.0000 | 0.0130 | 2.3930 | 20.0000 | AID593136 |
| P2Y purinoceptor 2 | Homo sapiens (human) | EC50 (µMol) | 0.2100 | 0.0056 | 0.6828 | 10.0000 | AID280297; AID404832; AID460573 |
| P2Y purinoceptor 4 | Homo sapiens (human) | EC50 (µMol) | 0.1400 | 0.0230 | 1.3623 | 10.0000 | AID404834 |
| P2Y purinoceptor 6 | Homo sapiens (human) | EC50 (µMol) | 0.9500 | 0.0130 | 2.3930 | 20.0000 | AID404830 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Biological Processes (21)
Molecular Functions (9)
Ceullar Components (5)
Bioassays (12)
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID593136 | Agonist activity at P2Y6 receptor | 2011 | Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8 | Structural modifications of UMP, UDP, and UTP leading to subtype-selective agonists for P2Y2, P2Y4, and P2Y6 receptors. |
| AID593135 | Agonist activity at P2Y4 receptor | 2011 | Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8 | Structural modifications of UMP, UDP, and UTP leading to subtype-selective agonists for P2Y2, P2Y4, and P2Y6 receptors. |
| AID593134 | Agonist activity at P2Y2 receptor | 2011 | Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8 | Structural modifications of UMP, UDP, and UTP leading to subtype-selective agonists for P2Y2, P2Y4, and P2Y6 receptors. |
| AID404832 | Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay | 2008 | Bioorganic & medicinal chemistry, Jun-15, Volume: 16, Issue:12 | Synthesis and potency of novel uracil nucleotides and derivatives as P2Y2 and P2Y6 receptor agonists. |
| AID404834 | Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay | 2008 | Bioorganic & medicinal chemistry, Jun-15, Volume: 16, Issue:12 | Synthesis and potency of novel uracil nucleotides and derivatives as P2Y2 and P2Y6 receptor agonists. |
| AID404830 | Agonist activity at human P2Y6 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay | 2008 | Bioorganic & medicinal chemistry, Jun-15, Volume: 16, Issue:12 | Synthesis and potency of novel uracil nucleotides and derivatives as P2Y2 and P2Y6 receptor agonists. |
| AID280297 | Agonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C | 2007 | Journal of medicinal chemistry, Mar-22, Volume: 50, Issue:6 | Molecular modeling of the human P2Y2 receptor and design of a selective agonist, 2'-amino-2'-deoxy-2-thiouridine 5'-triphosphate. |
| AID460573 | Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assay | 2010 | Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4 | 5-OMe-UDP is a potent and selective P2Y(6)-receptor agonist. |
| AID1346348 | Human P2Y4 receptor (P2Y receptors) | 2002 | The Journal of pharmacology and experimental therapeutics, Sep, Volume: 302, Issue:3 | Pharmacology of INS37217 [P(1)-(uridine 5')-P(4)- (2'-deoxycytidine 5')tetraphosphate, tetrasodium salt], a next-generation P2Y(2) receptor agonist for the treatment of cystic fibrosis. |
| AID1347028 | Human P2Y2 receptor (P2Y receptors) | 1996 | British journal of pharmacology, Jan, Volume: 117, Issue:1 | Enzymatic synthesis of UTP gamma S, a potent hydrolysis resistant agonist of P2U-purinoceptors. |
| AID1347028 | Human P2Y2 receptor (P2Y receptors) | 2001 | Bioorganic & medicinal chemistry letters, Jan-22, Volume: 11, Issue:2 | Synthesis and P2Y receptor activity of a series of uridine dinucleoside 5'-polyphosphates. |
| AID1347028 | Human P2Y2 receptor (P2Y receptors) | 2002 | The Journal of pharmacology and experimental therapeutics, Sep, Volume: 302, Issue:3 | Pharmacology of INS37217 [P(1)-(uridine 5')-P(4)- (2'-deoxycytidine 5')tetraphosphate, tetrasodium salt], a next-generation P2Y(2) receptor agonist for the treatment of cystic fibrosis. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
Research
Studies (30)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 1 (3.33) | 18.2507 |
| 2000's | 18 (60.00) | 29.6817 |
| 2010's | 11 (36.67) | 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: 12.99
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 (12.99) All Compounds (24.57) |
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 6 (23.08%) | 5.53% |
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 6 (23.08%) | 6.00% |
| Reviews | 0 (0.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 14 (53.85%) | 84.16% |
| Other | 6 (100.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||