1. Membrane Transporter/Ion Channel
  2. Potassium Channel
  3. Senicapoc

Senicapoc (Synonyms: ICA-17043)

Cat. No.: HY-50694 Purity: 99.83%
Handling Instructions

Senicapoc (ICA-17043) is a potent and selective Gardos channel blocker with IC50 value of 11 nM. 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.

For research use only. We do not sell to patients.

Senicapoc Chemical Structure

Senicapoc Chemical Structure

CAS No. : 289656-45-7

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10 mM * 1 mL in DMSO USD 119 In-stock
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100 mg USD 288 In-stock
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Customer Review

Based on 8 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Senicapoc purchased from MCE. Usage Cited in: J Cancer. 2017 Jun 3;8(9):1568-1578.

    H&E staining and Ki-67 immunohistochemistry of the respective tumors in two groups are performed.

    Senicapoc purchased from MCE. Usage Cited in: Eur J Pharmacol. 2017 Jan 15;795:1-7.

    In a second cohort of rats, the 50% paw withdrawal threshold (g) in response to von Frey stimulation of the injured hind paw is determined in CCI rats (n=12/group) dosed with either vehicle, senicapoc (SEN) or gabapentin (GBP). The efficacy of Senicapoc (10, 30 and 100 mg/kg, p.o.) is evaluated at its Tmax, 4 h after dosing.
    • Biological Activity

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    Description

    Senicapoc (ICA-17043) is a potent and selective Gardos channel blocker with IC50 value of 11 nM. 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.

    IC50 & Target

    IC50: 11 nM (Gardos channel)

    In Vitro

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

    In Vivo

    ICA-17043 (10 mg/kg, p.o.) 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. ICA-17043 (10 mg/kg, twice a day) induces a significant increase in Hct after 11 days of dosing in the SAD mouse[1]. Senicapoc (30 mg/kg, p.o.) reduces airway hyperresponsiveness, eosinophil numbers in bronchoalveolar lavage taken 48 hours post-allergen challenge, and vascular remodelling in the sheep[2].

    Clinical Trial
    Molecular Weight

    323.34

    Formula

    C₂₀H₁₅F₂NO

    CAS No.

    289656-45-7

    SMILES

    O=C(C(C1=CC=CC=C1)(C2=CC=C(C=C2)F)C3=CC=C(F)C=C3)N

    Shipping

    Room temperature in continental US; may vary elsewhere

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (154.64 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.0927 mL 15.4636 mL 30.9272 mL
    5 mM 0.6185 mL 3.0927 mL 6.1854 mL
    10 mM 0.3093 mL 1.5464 mL 3.0927 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (7.73 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (7.73 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (7.73 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
    Cell Assay
    [1]

    The whole blood is initially diluted 1:1 with Modified Flux Buffer (MFB), consisting of 140 mM NaCl, 5 mM KCl, 10 mM Tris (tris(hydroxymethyl)aminomethane), 0.1 mM EGTA (ethyleneglycoltetraacetic acid) (pH=7.4). The blood is centrifuged at 1000 rpm, and the pellet comprised primarily of RBCs is washed 3 times with MFB. The cells are then loaded with 86Rb+ by incubating the washed cells with 86Rb+ at a final concentration of 0.185 MBq/mL (5 μCi/mL) in MFB for at least 3 hours at 37°C. After loading with 86Rb+, the RBCs are washed 3 times with chilled MFB. The cells are then incubated for 10 minutes with test compound (senicapoc) at concentrations that ranged from 1 nM to 10 000 nM. Efflux of 86Rb+ is initiated by raising intracellular calcium levels in the RBCs with the addition of CaCl2 and A23187 (a calcium ionophore) to final concentrations of 2 mM and 5 μM, respectively. After 10 minutes of incubation at room temperature, the RBCs are pelleted in a microcentrifuge, and the supernatant is removed and counted in a Wallac MicroBeta liquid scintillation counter. 

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [1]

    Transgenic Hbbsingle/single SAD1 (SAD) female and male mice between 3 and 6 months of age, weighing 25 to 30 g, are used for this study. The SAD mice are divided into 2 groups, and either vehicle (n=6) or senicapoc (10 mg/kg) (n=6) is administered orally by gavage twice daily. C57B6/2J mice are used as controls (wild-type mice). Hematologic parameters are evaluated at baseline and after 11 and 21 days of therapy. Blood sampling and vehicle administration have previously been shown not to affect the blood parameters measured in this study.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
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    Product Name:
    Senicapoc
    Cat. No.:
    HY-50694
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