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Senicapoc (ICA-17043) Potassium Channel inhibitor

Cat.No.E0501

As a Gardos channel(Ca2+-activated K+ channel; KCa3.1) blocker with an IC50 of 11 nM, Senicapoc (ICA-17043) produces dose-dependent increases in hemoglobin and decreases in markers of hemolysis. It 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) Potassium Channel inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 323.34

Quality Control

Chemical Information, Storage & Stability

Molecular Weight 323.34 Formula

C20H15F2NO

Storage (From the date of receipt) 3 years -20°C powder
CAS No. 289656-45-7 -- Storage of Stock Solutions

Solubility

In vitro
Batch:

DMSO : 65 mg/mL (201.02 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 6 mg/mL

Water : Insoluble

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Mass Concentration Volume Molecular Weight

In vivo
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Mechanism of Action

Targets/IC50/Ki
KCa3.1 [1]
11 nM
In vitro

Senicapoc (ICA-17043) is shown to block the Gardos channel of mouse (C57 Black) RBCs with an IC50 of 50±6 nM. This compound also blocks the increase in cellular hemoglobin concentration in human RBCs in a concentration-dependent fashion.[1]

In vivo

Administration of Senicapoc (ICA-17043) 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. This compound (10 mg/kg, twice a day) induces a significant increase in Hct after 11 days of dosing in the SAD mouse.[1]

References

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