Lisofylline is a synthetic xanthine derivative with bronchodilator and anti-inflammatory properties. It is structurally similar to theophylline, another xanthine derivative, but with a unique chemical structure. It is studied for its potential therapeutic benefits in respiratory diseases like asthma and chronic obstructive pulmonary disease (COPD). Lisofylline acts as a phosphodiesterase (PDE) inhibitor, leading to increased levels of cyclic adenosine monophosphate (cAMP) in cells. This increased cAMP levels contribute to bronchodilation, reducing airway inflammation and improving lung function. Its specific mechanism of action involves inhibiting PDE4, which is primarily expressed in inflammatory cells. By inhibiting PDE4, lisofylline suppresses the production of pro-inflammatory mediators, such as cytokines and leukotrienes. This, in turn, helps to reduce airway inflammation and improve respiratory symptoms.'
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1-(5-hydroxyhexyl)-3,7-dimethylxanthine: the primary metabolite of pentoxifyline; CTP-499 is a partially deuterated form
1-(5-hydroxyhexyl)-3,7-dimethyl-3,7-dihydro-1H-purine-2,6-dione : A dimethylxanthine that is 3,7-dihydro-1H-purine-2,6-dione which is substituted at positions 1,3 and 7 by a 5-hydroxyhexyl group, methyl group and methyl group, respectively.
lisofylline: metabolite of pentoxifylline; structure given in first source
(R)-lisofylline : A 1-(5-hydroxyhexyl)-3,7-dimethyl-3,7-dihydro-1H-purine-2,6-dione that has (R)-configuration. A synthetic small molecule which was under development for the treatment of type 1 diabetes mellitus.
ID Source | ID |
---|---|
PubMed CID | 57782 |
CHEMBL ID | 1514176 |
CHEBI ID | 143565 |
SCHEMBL ID | 680306 |
MeSH ID | M0084266 |
PubMed CID | 501254 |
CHEMBL ID | 1411 |
CHEBI ID | 143527 |
SCHEMBL ID | 39131 |
MeSH ID | M0084266 |
Synonym |
---|
xanthine, 1-(5'-hydroxyhexyl)-3,7-dimethyl |
lsf |
SMP2_000274 |
NCGC00163298-01 |
3,7-dimethyl-1-(5-hydroxyhexyl)xanthine |
lisofylline [usan:inn] |
1-(5-hydroxyhexyl)-3,7-dimethyl-3,7-dihydro-1h-purine-2,6-dione |
1h-purine-2,6-dione, 3,7-dihydro-1-(5-hydroxyhexyl)-3,7-dimethyl- |
1-(5'-hydroxyhexyl)-3,7-dimethylxanthine |
bl 194 |
1h-purine-2,6-dione, 3,7-dihydro-1-(5-hydroxyhexyl)-3,7-dimethyl-, (r)- |
1-(5r-hydroxyhexyl)-3,7-dimethylxanthine |
1-(5-hydroxyhexyl)-3,7-dimethylpurine-2,6-dione |
pentoxifylline alcohol |
hydroxy pentoxifylline |
(+/-)-1-(5-hydroxyhexyl)-3,7-dimethylxanthine |
CHEBI:143565 |
lisophylline |
(+/-)-lisofylline |
(r)-lisophylline |
l1f2q2x956 , |
unii-l1f2q2x956 |
dtxsid6046343 , |
dtxcid4026343 |
cas-6493-06-7 |
tox21_112043 |
6493-06-7 |
lisofylline, (+/-)- |
theobromine, 1-(5-hydroxyhexyl)- |
penthydroxyfylline |
r99ee080js , |
penthydroxyfylline alcohol |
unii-r99ee080js |
FT-0670822 |
FT-0670823 |
5-hydroxypentoxyfylline |
5'-hydroxypentoxyphylline |
bl-194 |
hydroxypentoxifylline |
1h-purine-2,6-dione, 3,7-dihydro-1-(5-hydroxyhexyl)-3,7-dimethyl-theobromine, 1-(5-hydroxyhexyl)- |
(+/-)-lisophylline |
SCHEMBL680306 |
NCGC00163298-02 |
tox21_112043_1 |
CHEMBL1514176 |
mfcd00871850 |
(+/-)-lisofylline, analytical standard |
HY-126042 |
1-(5-hydroxyhexyl)-3,7-dimethylxanthine |
1-(5-hydroxyhexyl)-3,7-dimethyl-1h-purine-2,6(3h,7h)-dione |
FT-0670824 |
SB18959 |
AS-6130 |
1-[5-hydroxyhexyl]-3,7-dimethyl-3,7-dihydro-1h-purine-2,6-dione |
alcool metabolite, pentoxifylline |
6493-06-7 (racemic) |
lisofylline (raceimic) |
Q27288004 |
AT25342 |
( inverted exclamation marka)-lisofylline |
AKOS037645541 |
1-(5-hydroxyhexyl)-3,7-dimethyl-2,3,6,7-tetrahydro-1h-purine-2,6-dione |
lisofylline (r,s) |
penthydroxifillyne |
also see |
CS-0090310 |
ct1501r |
1-[(5r)-5-hydroxyhexyl]-3,7-dimethyl-purine-2,6-dione |
ct-1501r |
r-1-(5-hydroxyhexyl)-3,7-dimethylxanthine |
lisofylline |
protec |
protec (tn) |
lisofylline (usan/inn) |
D04748 |
100324-81-0 |
ct 1501r |
1-[(5r)-5-hydroxyhexyl]-3,7-dimethylpurine-2,6-dione |
CHEMBL1411 |
lisofylline, (r)- |
3,7-dihydro-1-[(5r)-5-hydroxyhexyl]-3,7-dimethyl-1h-purine-2,6-dione |
1-[(r)-5-hydroxyhexyl]theobromine |
CHEBI:143527 |
(r)-lsf |
1-[(5r)-5-hydroxyhexyl]-3,7-dimethyl-3,7-dihydro-1h-purine-2,6-dione |
1-[(5r)-5-hydroxyhexyl]-3,7-dimethyl-2,3,6,7-tetrahydro-1h-purine-2,6-dione |
(-)-lisofylline |
lisofyllinum |
lisofilina |
(r)-1-(5-hydroxyhexyl)-3,7-dimethylxanthine |
(r)-lisofylline |
NCGC00186630-01 |
SCHEMBL39131 |
lisofylline [usan] |
lisofylline [inn] |
lisofylline [mi] |
lisofylline [who-dd] |
DTXSID7058709 |
gtpl9225 |
AKOS025394050 |
J-000102 |
1-(5-r-hydroxyhexyl)-3,7-dimethylxanthine |
DB12406 |
HY-109854A |
Q15409404 |
CS-0034091 |
(r)-1-(5-hydroxyhexyl)-3,7-dimethyl-1h-purine-2,6(3h,7h)-dione |
MS-23979 |
EX-A6722 |
Excerpt | Reference | Relevance |
---|---|---|
" CTP-499 was well tolerated with no serious or severe adverse events, or adverse events leading to discontinuation." | ( A First-in-Patient, Multicenter, Double-Blind, 2-Arm, Placebo-Controlled, Randomized Safety and Tolerability Study of a Novel Oral Drug Candidate, CTP-499, in Chronic Kidney Disease. Braman, V; Cheng, C; Dao, M; Graham, P; Liu, J; Neutel, J; Sabounjian, L; Shipley, J; Wu, L, 2016) | 0.43 |
Lisofylline (LSF) is an anti-inflammatory molecule with high aqueous solubility and rapid metabolic interconversion to its parent drug. The aim of this study was to develop pharmacokinetic models for pentoxifylline (PTX) and the R(-)-enantiomer of the PTX metabolite 1,.
Excerpt | Reference | Relevance |
---|---|---|
" The pharmacokinetic parameters evaluated were area under the concentration-time curve from time zero extrapolated to infinity (AUC(0-infinity)), maximum concentration (Cmax), time to maximum concentration (Tmax), elimination rate constant (k(el)), and half-life (t1/2)." | ( Pharmacokinetics of intranasal and intratracheal pentoxifylline in rabbits. Adcock, KG; Deaton, JS; Hogan, SM; Kyle, PB; Olivier, JH, 2007) | 0.34 |
"The pharmacokinetic profiles after intranasal and intratracheal administration of pentoxifylline appear similar to those after intravenous administration." | ( Pharmacokinetics of intranasal and intratracheal pentoxifylline in rabbits. Adcock, KG; Deaton, JS; Hogan, SM; Kyle, PB; Olivier, JH, 2007) | 0.34 |
"The aim of this study was to develop pharmacokinetic models for pentoxifylline (PTX) and the R(-)-enantiomer of the PTX metabolite 1, lisofylline (LSF), in order to identify some factors influencing the absorption of these compounds from the intestines and to clarify mechanisms involved in their non-linear pharmacokinetics." | ( Pharmacokinetic modelling of pentoxifylline and lisofylline after oral and intravenous administration in mice. Obruśnik, A; Pekala, E; Szymura-Oleksiak, J; Wyska, E, 2007) | 0.34 |
" The application of the assay to a pilot pharmacokinetic study and tissue distribution of the compounds in rats after intraperitoneal dosing of 50 mg x kg(-1) of PTX was described." | ( Validation of a high-performance liquid chromatography method for pharmacokinetic evaluation of pentoxifylline and lisofylline in rat serum and tissues. Pekala, E; Szymura-Oleksiak, J; Walczak, M, ) | 0.13 |
" This hypothesis was supported by the outcomes of pharmacokinetic analysis." | ( Pharmacokinetic interaction between verapamil and methylxanthine derivatives in mice. Wyska, E, 2010) | 0.36 |
" The aim of the study was to develop a physiologically based pharmacokinetic (PBPK) model of LSF in mice and to perform simulations in order to predict LSF concentrations in human serum and tissues following intravenous and oral administration." | ( Physiologically based modeling of lisofylline pharmacokinetics following intravenous administration in mice. Pociecha, K; Przejczowska-Pomierny, K; Świerczek, A; Wyska, E, 2016) | 0.43 |
"Lisofylline (LSF) is an anti-inflammatory molecule with high aqueous solubility and rapid metabolic interconversion to its parent drug, pentoxifylline (PTX) resulting in very poor pharmacokinetic (PK) parameters, necessitating high dose and dosing frequency." | ( Nanoparticulate tablet dosage form of lisofylline-linoleic acid conjugate for type 1 diabetes: in situ single-pass intestinal perfusion (SPIP) studies and pharmacokinetics in rat. Chitkara, D; Italiya, KS; Mittal, A; Singh, AK, 2021) | 0.62 |
Lisofylline (LSF) is an anti-inflammatory molecule with high aqueous solubility and rapid metabolic interconversion to its parent drug, pentoxifylline (PTX) It has poor pharmacokinetic (PK) parameters, necessitating high dose and dosing frequency.
Excerpt | Relevance | Reference |
---|---|---|
"Prospective, randomized, and blinded survival studies were performed with two lisofylline dosing regimens added to fluid resuscitation in a shock model." | ( Lisofylline decreases white cell adhesiveness and improves survival after experimental hemorrhagic shock. Aswani, S; Daughters, K; Rice, G; Waxman, K, 1996) | 0.29 |
" Dosing was continued for 20 days or until the patient achieved 48 hrs of unassisted breathing." | ( Randomized, placebo-controlled trial of lisofylline for early treatment of acute lung injury and acute respiratory distress syndrome. , 2002) | 0.31 |
" These data provide support for development of pentoxifylline intranasal and intratracheal dosage formulations that would be suitable for use in premature neonates." | ( Pharmacokinetics of intranasal and intratracheal pentoxifylline in rabbits. Adcock, KG; Deaton, JS; Hogan, SM; Kyle, PB; Olivier, JH, 2007) | 0.34 |
" The application of the assay to a pilot pharmacokinetic study and tissue distribution of the compounds in rats after intraperitoneal dosing of 50 mg x kg(-1) of PTX was described." | ( Validation of a high-performance liquid chromatography method for pharmacokinetic evaluation of pentoxifylline and lisofylline in rat serum and tissues. Pekala, E; Szymura-Oleksiak, J; Walczak, M, ) | 0.13 |
" The proposed PK/PD model allowed a better understanding of the pharmacological properties of both methylxanthine derivatives and may be helpful in appropriate dosage selection for further studies." | ( Pharmacokinetic-pharmacodynamic modeling of methylxanthine derivatives in mice challenged with high-dose lipopolysaccharide. Wyska, E, 2010) | 0.36 |
"Lisofylline (LSF) is an anti-inflammatory molecule with high aqueous solubility and rapid metabolic interconversion to its parent drug, pentoxifylline (PTX) resulting in very poor pharmacokinetic (PK) parameters, necessitating high dose and dosing frequency." | ( Nanoparticulate tablet dosage form of lisofylline-linoleic acid conjugate for type 1 diabetes: in situ single-pass intestinal perfusion (SPIP) studies and pharmacokinetics in rat. Chitkara, D; Italiya, KS; Mittal, A; Singh, AK, 2021) | 0.62 |
Role | Description |
---|---|
anti-inflammatory agent | Any compound that has anti-inflammatory effects. |
immunomodulator | Biologically active substance whose activity affects or plays a role in the functioning of the immune system. |
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] |
Class | Description |
---|---|
secondary alcohol | A secondary alcohol is a compound in which a hydroxy group, -OH, is attached to a saturated carbon atom which has two other carbon atoms attached to it. |
dimethylxanthine | |
1-(5-hydroxyhexyl)-3,7-dimethyl-3,7-dihydro-1H-purine-2,6-dione | A dimethylxanthine that is 3,7-dihydro-1H-purine-2,6-dione which is substituted at positions 1,3 and 7 by a 5-hydroxyhexyl group, methyl group and methyl group, respectively. |
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] |
Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
acetylcholinesterase | Homo sapiens (human) | Potency | 0.7762 | 0.0025 | 41.7960 | 15,848.9004 | AID1347398 |
progesterone receptor | Homo sapiens (human) | Potency | 33.4915 | 0.0004 | 17.9460 | 75.1148 | AID1346795 |
cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 38.9018 | 0.0123 | 7.9835 | 43.2770 | AID1645841 |
Inositol monophosphatase 1 | Rattus norvegicus (Norway rat) | Potency | 0.5012 | 1.0000 | 10.4756 | 28.1838 | AID1457 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID504749 | qHTS profiling for inhibitors of Plasmodium falciparum proliferation | 2011 | Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043 | Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
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. |
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. |
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. |
AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
AID1815370 | Antidiabetic activity against STZ-induced diabetic Wistar rat model assessed as decrease in fasting blood glucose level at 15 mg/kg, ip administered once daily for 5 weeks and measured after 3 weeks by glucometric analysis | 2021 | Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19 | Role of Chain Length and Degree of Unsaturation of Fatty Acids in the Physicochemical and Pharmacological Behavior of Drug-Fatty Acid Conjugates in Diabetes. |
AID1815353 | Clearance in Wistar rat at 15 mg/kg, iv measured after 24 hrs by HPLC analysis | 2021 | Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19 | Role of Chain Length and Degree of Unsaturation of Fatty Acids in the Physicochemical and Pharmacological Behavior of Drug-Fatty Acid Conjugates in Diabetes. |
AID1815345 | AUMC (0 to t) in Wistar rat at 15 mg/kg, iv measured after 24 hrs by HPLC analysis | 2021 | Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19 | Role of Chain Length and Degree of Unsaturation of Fatty Acids in the Physicochemical and Pharmacological Behavior of Drug-Fatty Acid Conjugates in Diabetes. |
AID267569 | Secretion of insulin in INS1 cells at 20 uM | 2006 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13 | Synthesis and biological evaluation of lisofylline (LSF) analogs as a potential treatment for Type 1 diabetes. |
AID1815343 | AUC (0 to infinity) in Wistar rat at 15 mg/kg, iv by HPLC analysis | 2021 | Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19 | Role of Chain Length and Degree of Unsaturation of Fatty Acids in the Physicochemical and Pharmacological Behavior of Drug-Fatty Acid Conjugates in Diabetes. |
AID1815347 | AUMC (0 to infinity) in Wistar rat at 15 mg/kg, iv by HPLC analysis | 2021 | Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19 | Role of Chain Length and Degree of Unsaturation of Fatty Acids in the Physicochemical and Pharmacological Behavior of Drug-Fatty Acid Conjugates in Diabetes. |
AID1815364 | Binding affinity to bovine serum albumin assessed as decrease in fluorescence intensity measured after 30 mins by fluorescence quenching method | 2021 | Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19 | Role of Chain Length and Degree of Unsaturation of Fatty Acids in the Physicochemical and Pharmacological Behavior of Drug-Fatty Acid Conjugates in Diabetes. |
AID1815337 | Initial plasma concentration in Wistar rat at 15 mg/kg, iv by HPLC analysis | 2021 | Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19 | Role of Chain Length and Degree of Unsaturation of Fatty Acids in the Physicochemical and Pharmacological Behavior of Drug-Fatty Acid Conjugates in Diabetes. |
AID1815351 | Volume of distribution in Wistar rat at 15 mg/kg, iv measured after 24 hrs by HPLC analysis | 2021 | Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19 | Role of Chain Length and Degree of Unsaturation of Fatty Acids in the Physicochemical and Pharmacological Behavior of Drug-Fatty Acid Conjugates in Diabetes. |
AID267568 | Protection of cytokine-induced death of pancreatic beta cells at 0.1 uM | 2006 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13 | Synthesis and biological evaluation of lisofylline (LSF) analogs as a potential treatment for Type 1 diabetes. |
AID1815341 | AUC (0 to t) in Wistar rat at 15 mg/kg, iv measured after 24 hrs by HPLC analysis | 2021 | Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19 | Role of Chain Length and Degree of Unsaturation of Fatty Acids in the Physicochemical and Pharmacological Behavior of Drug-Fatty Acid Conjugates in Diabetes. |
AID1815366 | Elimination rate constant in Wistar rat at 15 mg/kg,iv measured after 24 hrs by HPLC analysis | 2021 | Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19 | Role of Chain Length and Degree of Unsaturation of Fatty Acids in the Physicochemical and Pharmacological Behavior of Drug-Fatty Acid Conjugates in Diabetes. |
AID1815373 | Protection against STZ-induced pancreatic beta cell destruction in Wistar rat assessed as proper arrangement of islets at 15 mg/kg, ip administered once daily for 5 weeks and measured on day 35 by Hematoxylin and eosin staining based analysis | 2021 | Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19 | Role of Chain Length and Degree of Unsaturation of Fatty Acids in the Physicochemical and Pharmacological Behavior of Drug-Fatty Acid Conjugates in Diabetes. |
AID1815349 | MRT in Wistar rat at 15 mg/kg, iv measured after 24 hrs by HPLC analysis | 2021 | Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19 | Role of Chain Length and Degree of Unsaturation of Fatty Acids in the Physicochemical and Pharmacological Behavior of Drug-Fatty Acid Conjugates in Diabetes. |
AID267571 | Half life in human liver | 2006 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13 | Synthesis and biological evaluation of lisofylline (LSF) analogs as a potential treatment for Type 1 diabetes. |
AID1815371 | Antidiabetic activity against STZ-induced diabetic Wistar rat model assessed as decrease in fasting blood glucose level at 15 mg/kg, ip administered once daily for 5 weeks and measured after 5 weeks by glucometric analysis | 2021 | Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19 | Role of Chain Length and Degree of Unsaturation of Fatty Acids in the Physicochemical and Pharmacological Behavior of Drug-Fatty Acid Conjugates in Diabetes. |
AID1815339 | Half life in Wistar rat at 15 mg/kg, iv measured after 24 hrs by HPLC analysis | 2021 | Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19 | Role of Chain Length and Degree of Unsaturation of Fatty Acids in the Physicochemical and Pharmacological Behavior of Drug-Fatty Acid Conjugates in Diabetes. |
AID1815332 | Cytotoxicity against mouse MIN6 cells assessed as cell viability at 20 uM equiv. LSF measured after 48 hrs by MTT assay | 2021 | Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19 | Role of Chain Length and Degree of Unsaturation of Fatty Acids in the Physicochemical and Pharmacological Behavior of Drug-Fatty Acid Conjugates in Diabetes. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 8 (7.14) | 18.7374 |
1990's | 38 (33.93) | 18.2507 |
2000's | 34 (30.36) | 29.6817 |
2010's | 23 (20.54) | 24.3611 |
2020's | 9 (8.04) | 2.80 |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
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 (25.31) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 1 (9.09%) | 5.53% |
Trials | 6 (5.71%) | 5.53% |
Reviews | 0 (0.00%) | 6.00% |
Reviews | 5 (4.76%) | 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 | 10 (90.91%) | 84.16% |
Other | 94 (89.52%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Trial | Phase | Enrollment | Study Type | Start Date | Status | ||
---|---|---|---|---|---|---|---|
A Safety, Tolerability and Bioavailability Study of Lisofylline After Continuous Subcutaneous (12 mg/kg) and Intravenous (12 mg/kg) Administration in Healthy Subjects and in Subjects With Type 1 Diabetes Mellitus [NCT00896077] | Phase 1/Phase 2 | 8 participants (Actual) | Interventional | 2009-05-31 | Completed | ||
Strategies to Improve Long Term Islet Graft Survival [NCT00464555] | Phase 2 | 5 participants (Actual) | Interventional | 2006-12-31 | Completed | ||
A Safety, Tolerability and Bioavailability Study of Lisofylline After Continuous Subcutaneous (12 mg/kg) and Intravenous (9 mg/kg) Administration in Subjects With Type 1 Diabetes Mellitus [NCT01603121] | Phase 1/Phase 2 | 1 participants (Actual) | Interventional | 2012-02-29 | Terminated(stopped due to Unable to enroll sufficient number of subjects) | ||
[information is prepared from clinicaltrials.gov, extracted Sep-2024] |