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Chemical Structure| 289656-45-7 Chemical Structure| 289656-45-7

Structure of Senicapoc
CAS No.: 289656-45-7

Chemical Structure| 289656-45-7

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Senicapoc is a potent and selective Gardos channel blocker and blocks Ca(2+)-induced rubidium flux from human RBCs/ inhibited RBC dehydration with IC50s of 11 nM/30 nM, respectively.

Synonyms: ICA-17043

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Product Details of Senicapoc

CAS No. :289656-45-7
Formula : C20H15F2NO
M.W : 323.34
SMILES Code : O=C(N)C(C1=CC=C(F)C=C1)(C2=CC=C(F)C=C2)C3=CC=CC=C3
Synonyms :
ICA-17043
MDL No. :MFCD09027349
InChI Key :SCTZUZTYRMOMKT-UHFFFAOYSA-N
Pubchem ID :216327

Safety of Senicapoc

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
mouse microglial cells 7 nM 24 h Senicapoc inhibited KCa3.1 currents, reduced ATP-induced Ca2+ signaling, and suppressed the expression of pro-inflammatory cytokines and enzymes. PMC11106165
WM266-4 cells 30 µM 72 h To evaluate the effect of Senicapoc on WM266-4 cell viability, results showed a significant decrease in cell viability PMC10671816
Panc-1 cells 30 µM 72 h To evaluate the effect of Senicapoc on Panc-1 cell viability, results showed a significant decrease in cell viability PMC10671816
human CD3+ T cells 100 nM, 250 nM, 1 µM 48 h To study the effect of Senicapoc on T cell proliferation and cytokine production, results showed that Senicapoc decreased the production of IL-2, IFN-γ, IL-12, and IL-17A, but not TNF-α and IL-10 PMC4216648
BDKO cells 0.5 µM 4 min significantly blocked Tmem63b-mediated PLS PMC11366033

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6J mice transient middle cerebral artery occlusion model intraperitoneal injection 10 mg/kg and 40 mg/kg every 12 hours for a total of 14 doses Senicapoc significantly reduced infarct area, improved neurological deficits, and decreased microglia/macrophage and T cell infiltration and activation. PMC11106165
Mice KCa3.1-overexpressing mice Chow administration 30 mg/day Once daily for 2 weeks Senicapoc treatment prevented the intestinal phenotype in KCa3.1-overexpressing mice, including changes in water intake, frequency, and amplitude of duodenal contractions. PMC6429421
mice MPTP-induced Parkinson's disease model oral 100 mg/kg once daily for 5 days To study the effect of Senicapoc on MPTP-induced Parkinson's disease model, results showed that Senicapoc improved locomotor ability, increased TH-positive neuron number, and attenuated microglial activation and neuroinflammation PMC6931251

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT00102791 Sickle Cell Disease PHASE3 TERMINATED 2025-06-07 Mobile, Alabama, United States... More >>|Little Rock, Arkansas, United States|Davis, California, United States|Los Angeles, California, United States|Oakland, California, United States|Denver, Colorado, United States|Hartford, Connecticut, United States|Washington, District of Columbia, United States|Holly Hill, Florida, United States|Hollywood, Florida, United States|Jacksonville, Florida, United States|Augusta, Georgia, United States|Savannah, Georgia, United States|Chicago, Illinois, United States|Iowa City, Iowa, United States|New Orleans, Louisiana, United States|Shreveport, Louisiana, United States|Baltimore, Maryland, United States|Boston, Massachusetts, United States|Detroit, Michigan, United States|Jackson, Mississippi, United States|Kansas City, Missouri, United States|Las Vegas, Nevada, United States|Hackensack, New Jersey, United States|New Brunswick, New Jersey, United States|Newark, New Jersey, United States|Bronx, New York, United States|Brooklyn, New York, United States|Chapel Hill, North Carolina, United States|Durham, North Carolina, United States|Greenville, North Carolina, United States|Winston-Salem, North Carolina, United States|Cincinnati, Ohio, United States|Cleveland, Ohio, United States|Philadelphia, Pennsylvania, United States|Pittsburgh, Pennsylvania, United States|Charleston, South Carolina, United States|Memphis, Tennessee, United States|Nashville, Tennessee, United States|Houston, Texas, United States|San Antonio, Texas, United States|Richmond, Virginia, United States|Porto Alegre, Brazil|Rio de Janeiro, Brazil|Sao Paulo, Brazil|Creteil, France|Kingston, Jamaica|Port of Spain, Trinidad and Tobago|London, United Kingdom Less <<
NCT00294541 Sickle Cell Disease|Sickle Cel... More >>l Anemia Less << PHASE3 TERMINATED 2025-06-07 University of South Alabama, M... More >>obile, Alabama, 36617, United States|Arkansas Children's Hospital, Little Rock, Arkansas, 72202, United States|Children's Hospital Oakland, Oakland, California, 94609, United States|University of California Davis Medical Center, Sacramento, California, 95817, United States|University of Colorado Health Sciences Center, Denver, Colorado, 80262, United States|Century Clinical Research, Inc., Holly Hill, Florida, 32117, United States|University of Florida Health Science Center, Jacksonville, Florida, 32209, United States|Medical College of Georgia, Augusta, Georgia, 30912, United States|Memorial Health University Medical Center, Savannah, Georgia, 31404, United States|University of Illinois Medical Center, Chicago, Illinois, 60612, United States|Sickle Cell Center of Northern Louisiana, Shreveport, Louisiana, 71103, United States|Johns Hopkins University School of Medicine, Baltimore, Maryland, 21205, United States|Brigham and Women's Hospital, Boston, Massachusetts, 02115, United States|Wayne State School of Medicine, Detroit, Michigan, 48201, United States|University of Mississippi Medical Center, Jackson, Mississippi, 39216, United States|Hackensack University Medical Center, Hackensack, New Jersey, 07601, United States|Robert Wood Johnson Medical Center, New Brunswick, New Jersey, 08903, United States|Newark Beth Israel Medical Center, Newark, New Jersey, 07112-2027, United States|SUNY Downstate Medical Center, Brooklyn, New York, 11203, United States|New York Methodist Hospital, Brooklyn, New York, 11215, United States|University of North Carolina Hospitals, Chapel Hill, North Carolina, 27514, United States|Duke University Medical Center, Durham, North Carolina, 27710, United States|East Carolina University School of Medicine, Greenville, North Carolina, 27858, United States|Wake Forest University School of Medicine, Winston-Salem, North Carolina, 27157, United States|University of Cincinnati, Cincinnati, Ohio, 45219, United States|Thomas Jefferson University Hospital, Philadelphia, Pennsylvania, 19107, United States|St. Christopher's Hospital for Children, Philadelphia, Pennsylvania, 19134-1095, United States|Medical University of South Carolina, Charleston, South Carolina, 29425, United States|Baylor College of Medicine, Houston, Texas, 77030, United States|Medical College of Virginia, Richmond, Virginia, 23298-0157, United States|Virginia Commonwealth University, Richmond, Virginia, 23298, United States Less <<
NCT00040677 Sickle Cell Disease ... More >> Sickle Cell Anemia Less << Phase 2 Completed - United States, Alabama ... More >> Study Site Birmingham, Alabama, United States United States, California Study Site Oakland, California, United States Study Site San Francisco, California, United States United States, District of Columbia Study Site Washington, District of Columbia, United States United States, Georgia Study Site Augusta, Georgia, United States United States, Illinois Study Site Chicago, Illinois, United States United States, Maryland Study Site Baltimore, Maryland, United States United States, Massachusetts Study Site Boston, Massachusetts, United States United States, Michigan Study Site Detroit, Michigan, United States United States, Mississippi Study Site Jackson, Mississippi, United States United States, New York Study Site Brooklyn, New York, United States Study Site New York, New York, United States United States, North Carolina Study Site Chapel Hill, North Carolina, United States Study Site Durham, North Carolina, United States United States, Pennsylvania Study Site Philadelphia, Pennsylvania, United States Study Site Pittsburgh, Pennsylvania, United States United States, Tennessee Study Site Nashville, Tennessee, United States United States, Texas Study Site Houston, Texas, United States United States, Virginia Study Site Richmond, Virginia, United States Less <<
NCT00861211 Atopic Asthma Phase 2 Completed - United Kingdom ... More >> Guy's Drug Research Unit London, UK, United Kingdom, SE1 1YR Medicines Evaluation Unit Manchester, UK, United Kingdom, M23 9QZ Less <<
NCT00861185 Exercise Induced Asthma Phase 2 Completed - United States, California ... More >> Huntington Beach, California, United States, 92647 Orange, California, United States, 92868 United States, Illinois Normal, Illinois, United States, 61761 United States, Louisiana Metairie, Louisiana, United States, 70006 United States, Missouri St. Louis, Missouri, United States, 63141 United States, New Jersey Skillman, New Jersey, United States, 08558 United States, New York North Syracuse, New York, United States, 13212 United States, Ohio Canton, Ohio, United States, 44718 United States, Washington Seattle,, Washington, United States, 98105 Less <<
NCT04594668 ARDS, Human|COVID PHASE2 UNKNOWN 2021-12-31 Aalborg University Hospital, A... More >>alborg, 9000, Denmark|Aarhus University Hospital, Aarhus, 8000, Denmark|Hvidovre Hospital, Hvidovre, 2650, Denmark|Odense University Hospital, Odense, 5000, Denmark Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.09mL

0.62mL

0.31mL

15.46mL

3.09mL

1.55mL

30.93mL

6.19mL

3.09mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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