Page last updated: 2024-12-08
senicapoc
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Market Indicators
Description
senicapoc: a Gardos channel blocker; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
ID Source | ID |
---|---|
PubMed CID | 216327 |
CHEMBL ID | 405821 |
SCHEMBL ID | 1443805 |
MeSH ID | M0535758 |
Synonyms (46)
Synonym |
---|
HY-50694 |
ica17043 |
gtpl2331 |
senicapoc |
ica-17043 |
289656-45-7 |
senicapoc (usan) |
D06640 |
bis(4-fluorophenyl)phenylacetamide |
2,2-bis(4-fluorophenyl)-2-phenylacetamide |
CHEMBL405821 |
pf-05416266 |
FT-0660387 |
AKOS007930800 |
SCHEMBL1443805 |
A822267 |
2,2-bis(4-fluorophenyl)-2-phenyl-ethanamide |
unii-ts6g201a6q |
4-fluoro-alpha-(4-fluorophenyl)-alpha-phenylbenzeneacetamide |
benzeneacetamide, 4-fluoro-alpha-(4-fluorophenyl)-alpha-phenyl- |
ts6g201a6q , |
senicapoc [usan:inn] |
bdbm50371391 |
CS-0294 |
c20h15f2no |
senicapoc [inn] |
senicapoc [who-dd] |
senicapoc [usan] |
senicapoc [mart.] |
SCTZUZTYRMOMKT-UHFFFAOYSA-N |
ica 17043 |
DTXSID60276906 |
C74487 |
BBL102413 |
STL556215 |
4-methyl-1h-pyrrole-2-carboxylic?acid |
DB06280 |
BCP14507 |
Q7450628 |
mfcd09027349 |
AMY2744 |
MS-20434 |
HMS3741E13 |
AU-004/43508060 |
A904983 |
SY291889 |
Research Excerpts
Effects
Excerpt | Reference | Relevance |
---|---|---|
"Senicapoc, which has previously been in Phase III clinical trials, would be available for repurposing, and could be used to quickly translate findings made with other KCa3.1 blocking tool compounds into clinical trials." | ( KCa3.1 Channel Modulators as Potential Therapeutic Compounds for Glioblastoma. Brown, BM; Pressley, B; Wulff, H, 2018) | 1.92 |
Treatment
Senicapoc-treated sheep also demonstrated reduced airway hyperresponsiveness, requiring a significantly higher dose of carbachol to increase resistance by 100% compared to allergen-challenged vehicle-control sheep.
Toxicity
Excerpt | Reference | Relevance |
---|---|---|
" Finally, senicapoc was safe and well tolerated." | ( Efficacy and safety of the Gardos channel blocker, senicapoc (ICA-17043), in patients with sickle cell anemia. Ataga, KI; Castro, O; De Castro, LM; Kutlar, A; Orringer, EP; Rigdon, GC; Saunthararajah, Y; Smith, WR; Stocker, JW; Swerdlow, P; Vichinsky, E, 2008) | 1 |
Bioavailability
Excerpt | Reference | Relevance |
---|---|---|
" This study rationally devised strategies to increase drug bioavailability by increasing ocular surface residence time of drug-loaded nanoliposomes dispersed within thermo-sensitive hydrogels (Pluronic F-127)." | ( Topical Delivery of Senicapoc Nanoliposomal Formulation for Ocular Surface Treatments. Bose, T; Chandy, GK; Hou, A; Huang, Y; Lui, YS; Phua, JL; Tong, L; Venkatraman, S, 2018) | 0.8 |
Dosage Studied
Excerpt | Relevance | Reference |
---|---|---|
" With the long half-life of ICA-17043 demonstrated in this study, once-daily dosing is probably adequate to maintain steady-state plasma concentrations." | ( Dose-escalation study of ICA-17043 in patients with sickle cell disease. Ataga, KI; Davis, GA; Desimone, PA; Orringer, EP; Stocker, JW; Styles, L; Swerdlow, P; Vichinsky, EP, 2006) | 0.33 |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Protein Targets (11)
Inhibition Measurements
Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Intermediate conductance calcium-activated potassium channel protein 4 | Homo sapiens (human) | IC50 (µMol) | 3.6727 | 0.0060 | 0.0797 | 0.3600 | AID315276; AID726261; AID726263 |
Potassium voltage-gated channel subfamily A member 5 | Homo sapiens (human) | IC50 (µMol) | 1.0000 | 0.0300 | 3.7300 | 9.0000 | AID726259 |
Sodium channel protein type 1 subunit alpha | Homo sapiens (human) | IC50 (µMol) | 1.0000 | 0.0023 | 2.8296 | 9.0000 | AID726292 |
Sodium channel protein type 4 subunit alpha | Homo sapiens (human) | IC50 (µMol) | 1.0000 | 0.0001 | 3.5075 | 10.0000 | AID726289 |
Potassium voltage-gated channel subfamily KQT member 1 | Homo sapiens (human) | IC50 (µMol) | 1.0000 | 0.1200 | 4.0480 | 10.0000 | AID726258 |
Potassium voltage-gated channel subfamily H member 2 | Homo sapiens (human) | IC50 (µMol) | 1.0000 | 0.0009 | 1.9014 | 10.0000 | AID726260 |
Sodium channel protein type 9 subunit alpha | Homo sapiens (human) | IC50 (µMol) | 1.0000 | 0.0060 | 2.7749 | 9.0000 | AID726285 |
Sodium channel protein type 2 subunit alpha | Homo sapiens (human) | IC50 (µMol) | 1.0000 | 0.0000 | 3.7401 | 10.0000 | AID726290 |
Sodium channel protein type 3 subunit alpha | Homo sapiens (human) | IC50 (µMol) | 1.0000 | 0.0053 | 2.8085 | 9.0000 | AID726291 |
Sodium channel protein type 8 subunit alpha | Homo sapiens (human) | IC50 (µMol) | 1.0000 | 0.0011 | 3.4705 | 9.0000 | AID726288 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Biological Processes (117)
Molecular Functions (34)
Ceullar Components (51)
Bioassays (27)
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID726260 | Inhibition of human ERG channel | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3 | Ion channels as therapeutic targets: a drug discovery perspective. |
AID726261 | Inhibition of gardos channel (unknown origin) | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3 | Ion channels as therapeutic targets: a drug discovery perspective. |
AID726292 | Inhibition of voltage-gated Na channel 1.1 (unknown origin) | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3 | Ion channels as therapeutic targets: a drug discovery perspective. |
AID315297 | Effect on hematocrit levels in SAD1 mouse model at 10 mg/kg, po bid after 21 days | 2008 | Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4 | Novel inhibitors of the Gardos channel for the treatment of sickle cell disease. |
AID726289 | Inhibition of voltage-gated Na channel 1.4 (unknown origin) | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3 | Ion channels as therapeutic targets: a drug discovery perspective. |
AID315276 | Inhibition of Gardos channel in human RBC assessed as inhibition of ionomycin-stimulated [86Rb] efflux | 2008 | Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4 | Novel inhibitors of the Gardos channel for the treatment of sickle cell disease. |
AID726290 | Inhibition of voltage-gated Na channel 1.2 (unknown origin) | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3 | Ion channels as therapeutic targets: a drug discovery perspective. |
AID726288 | Inhibition of voltage-gated Na channel 1.6 (unknown origin) | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3 | Ion channels as therapeutic targets: a drug discovery perspective. |
AID315277 | Intrinsic clearance in rat liver microsome S9 fraction as % compound remaining after incubation | 2008 | Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4 | Novel inhibitors of the Gardos channel for the treatment of sickle cell disease. |
AID315294 | Effect on mean corpuscular hemoglobin concentration in SAD1 mouse model at 10 mg/kg, po bid after 11 days | 2008 | Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4 | Novel inhibitors of the Gardos channel for the treatment of sickle cell disease. |
AID315279 | Bioavailability in Sprague-Dawley rat at 1 mg/kg, iv or 10 mg/kg, po | 2008 | Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4 | Novel inhibitors of the Gardos channel for the treatment of sickle cell disease. |
AID315282 | Cmax in Sprague-Dawley rat at 1 mg/kg, iv or 10 mg/kg, po | 2008 | Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4 | Novel inhibitors of the Gardos channel for the treatment of sickle cell disease. |
AID726259 | Inhibition of voltage-gated K channel 1.5 (unknown origin) | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3 | Ion channels as therapeutic targets: a drug discovery perspective. |
AID315278 | Solubility by shake-flask method | 2008 | Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4 | Novel inhibitors of the Gardos channel for the treatment of sickle cell disease. |
AID315281 | Tmax in Sprague-Dawley rat at 1 mg/kg, iv or 10 mg/kg, po | 2008 | Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4 | Novel inhibitors of the Gardos channel for the treatment of sickle cell disease. |
AID726291 | Inhibition of voltage-gated Na channel 1.3 (unknown origin) | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3 | Ion channels as therapeutic targets: a drug discovery perspective. |
AID726263 | Inhibition of Kca 3.1 (unknown origin) | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3 | Ion channels as therapeutic targets: a drug discovery perspective. |
AID726285 | Inhibition of voltage-gated Na channel 1.7 (unknown origin) | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3 | Ion channels as therapeutic targets: a drug discovery perspective. |
AID315280 | Half life in Sprague-Dawley rat at 1 mg/kg, iv or 10 mg/kg, po | 2008 | Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4 | Novel inhibitors of the Gardos channel for the treatment of sickle cell disease. |
AID315284 | Inhibition of CYP3A4 at 10 uM | 2008 | Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4 | Novel inhibitors of the Gardos channel for the treatment of sickle cell disease. |
AID315293 | Effect on gardos channel activity in SAD1 mouse model at 10 mg/kg, po bid after 21 days | 2008 | Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4 | Novel inhibitors of the Gardos channel for the treatment of sickle cell disease. |
AID315296 | Effect on hematocrit levels in SAD1 mouse model at 10 mg/kg, po bid after 11 days | 2008 | Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4 | Novel inhibitors of the Gardos channel for the treatment of sickle cell disease. |
AID315295 | Effect on mean corpuscular hemoglobin concentration in SAD1 mouse model at 10 mg/kg, po bid after 21 days | 2008 | Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4 | Novel inhibitors of the Gardos channel for the treatment of sickle cell disease. |
AID726258 | Inhibition of voltage-gated K channel 7.1 (unknown origin) | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3 | Ion channels as therapeutic targets: a drug discovery perspective. |
AID315292 | Effect on gardos channel activity in SAD1 mouse model at 10 mg/kg, po bid after 11 days | 2008 | Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4 | Novel inhibitors of the Gardos channel for the treatment of sickle cell disease. |
AID726257 | Inhibition of IK (unknown origin) | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3 | Ion channels as therapeutic targets: a drug discovery perspective. |
AID1346444 | Human KCa3.1 (Calcium- and sodium-activated potassium channels) | 2003 | Blood, Mar-15, Volume: 101, Issue:6 | ICA-17043, a novel Gardos channel blocker, prevents sickled red blood cell dehydration in vitro and in vivo in SAD mice. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Research
Studies (41)
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 0 (0.00) | 18.2507 |
2000's | 8 (19.51) | 29.6817 |
2010's | 23 (56.10) | 24.3611 |
2020's | 10 (24.39) | 2.80 |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Market Indicators
Research Demand Index: 30.79
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 (30.79) All Compounds (24.57) |
Study Types
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 3 (7.14%) | 5.53% |
Reviews | 10 (23.81%) | 6.00% |
Case Studies | 0 (0.00%) | 4.05% |
Observational | 0 (0.00%) | 0.25% |
Other | 29 (69.05%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |