Home Transmembrane Transporters Potassium Channel inhibitor Senicapoc (ICA-17043) For research use only.

Senicapoc (ICA-17043)

Senicapoc (ICA-17043) is a Gardos channel(Ca2+-activated K+ channel; KCa3.1) blocker with an IC50 of 11 nM and produces dose-dependent increases in hemoglobin and decreases in markers of hemolysis. Senicapoc blocks Ca2+-induced rubidium flux from human RBCs with an IC50 value of 11 nM and inhibits RBC dehydration with IC50 of 30 nM.

Senicapoc (ICA-17043) Chemical Structure

Senicapoc (ICA-17043) Chemical Structure

CAS No. 289656-45-7

Purity & Quality Control

Senicapoc (ICA-17043) Related Products

Signaling Pathway

Potassium Channel Signaling Pathways

Potassium Channel Signaling Pathway

Biological Activity

Description Senicapoc (ICA-17043) is a Gardos channel(Ca2+-activated K+ channel; KCa3.1) blocker with an IC50 of 11 nM and produces dose-dependent increases in hemoglobin and decreases in markers of hemolysis. Senicapoc blocks Ca2+-induced rubidium flux from human RBCs with an IC50 value of 11 nM and inhibits RBC dehydration with IC50 of 30 nM.
Targets
KCa3.1 [1]
11 nM
In vitro
In vitro

Senicapoc (ICA-17043) is shown to block the Gardos channel of mouse (C57 Black) RBCs with an IC50 of 50±6 nM.Senicapoc blocks this increase in cellular hemoglobin concentration in human RBCs in a concentration-dependent fashion.[1]
Cell Research Cell lines Human RBCs
Concentrations 1 nM-10 mM, 10 μM
Incubation Time 10 min
Method

Heparinized human blood is centrifuged at 2000 rpm, and the resulting pellet is washed 3 times with MFB as described previously. The RBC pellet is resuspended in MFB. Senicapoc, at increasing concentrations, is incubated with an aliquot of cells for 10 minutes at room temperature.
In Vivo
In vivo

Senicapoc (ICA-17043) administration produces a significant decrease in Gardos channel activity measured at day 11 and 21 and is associated with a corresponding increase in red cell K+ content without changes in Na+ content. Senicapoc (10 mg/kg, twice a day) induces a significant increase in Hct after 11 days of dosing in the SAD mouse.[1]
Animal Research Animal Models SAD mouse, Transgenic Hbb SAD1 mice
Dosages 10 mg/kg
Administration p.o.

Chemical Information & Solubility

Molecular Weight 323.34 Formula

C20H15F2NO
CAS No. 289656-45-7 SDF --
Smiles NC(=O)C(C1=CC=CC=C1)(C2=CC=C(F)C=C2)C3=CC=C(F)C=C3
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 65 mg/mL ( (201.02 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 6 mg/mL

Water : Insoluble


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In vivo
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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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