Senicapoc (ICA-17043)

Catalog No.E0501 Batch:E050101

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Technical Data

Formula

C20H15F2NO
Molecular Weight 323.34 CAS No. 289656-45-7
Solubility (25°C)* In vitro DMSO 65 mg/mL (201.02 mM)
Ethanol 6 mg/mL (18.55 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
2%DMSO 40%PEG300 5%Tween80 53%ddH2O
1.0mg/ml Taking the 1 mL working solution as an example, add 20 μL of 50 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 530 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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

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]
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]

Protocol (from reference)

Cell Assay:

[1]
  • 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.
Animal Study:

[1]
  • Animal Models

    SAD mouse, Transgenic Hbb SAD1 mice

  • Dosages

    10 mg/kg

  • Administration

    p.o.

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.