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Senicapoc

Catalog No. T3528   CAS 289656-45-7
Synonyms: ICA-17043

Senicapoc (ICA-17043) is a potent inhibitor of the Gardos channel and ameliorates RBC dehydration in the SAD mouse. Senicapoc blocked Ca2+-induced rubidium flux from human RBCs with an IC50 value of 11 ± 2 nM (CLT IC50 = 100 ± 12 nM) and inhibited RBC dehydration with an IC50 of 30 ± 20 nM. Senicapoc is in treatment of Sickle Cell Disease and Sickle Cell Anemia

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Senicapoc Chemical Structure
Senicapoc, CAS 289656-45-7
Pack Size Availability Price/USD Quantity
5 mg In stock $ 54.00
10 mg In stock $ 87.00
25 mg In stock $ 135.00
50 mg In stock $ 177.00
100 mg In stock $ 237.00
200 mg In stock $ 353.00
1 mL * 10 mM (in DMSO) In stock $ 65.00
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Purity: 99.5%
Purity: 95.7%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Senicapoc (ICA-17043) is a potent inhibitor of the Gardos channel and ameliorates RBC dehydration in the SAD mouse. Senicapoc blocked Ca2+-induced rubidium flux from human RBCs with an IC50 value of 11 ± 2 nM (CLT IC50 = 100 ± 12 nM) and inhibited RBC dehydration with an IC50 of 30 ± 20 nM. Senicapoc is in treatment of Sickle Cell Disease and Sickle Cell Anemia
Targets&IC50 RBC:30 ± 20 nM, human RBCs:11 ± 2 nM
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].
Cell Research Senicapoc is dissolved in DMSO or 100% ethanol. 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.
Synonyms ICA-17043
Molecular Weight 323.34
Formula C20H15F2NO
CAS No. 289656-45-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (154.64 mM), sonification is recommended.

TargetMolReferences and Literature

1. Stocker JW, et al. ICA-17043, a novel Gardos channel blocker, prevents sickled red blood cell dehydration in vitro and in vivo in SAD mice. Blood. 2003 Mar 15;101(6):2412-8. 2. Van Der Velden J, et al. K(Ca)3.1 channel-blockade attenuates airway pathophysiology in a sheep model of chronic asthma. PLoS One. 2013 Jun 24;8(6):e66886. 3. Gong X, Zou L, Wang M, et al. Gramicidin inhibits cholangiocarcinoma cell growth by suppressing EGR4[J]. Artificial Cells, Nanomedicine, and Biotechnology. 48(1): 53-59. 4. Wei T, Wang Y, Xu W, et al. KCa3. 1 deficiency attenuates neuroinflammation by regulating an astrocyte phenotype switch involving the PI3K/AKT/GSK3β pathway[J]. Neurobiology of Disease. 2019: 104588.

TargetMolCitations

1. Lu J, Dou F, Yu Z. The potassium channel KCa3.1 represents a valid pharmacological target for microgliosis-induced neuronal impairment in a mouse model of Parkinson’s disease. Journal of Neuroinflammation. 2019, 16(1): 1-14 2. Wei T, Wang Y, Xu W, et al. KCa3.1 deficiency attenuates neuroinflammation by regulating an astrocyte phenotype switch involving the PI3K/AKT/GSK3β pathway. Neurobiology of Disease. 2019, 132: 104588 3. Gong X, Zou L, Wang M, et al. Gramicidin inhibits cholangiocarcinoma cell growth by suppressing EGR4. Artificial Cells, Nanomedicine, and Biotechnology. 48(1): 53-59.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Clinical Compound Library Potassium Channel Blocker Library Hematonosis Compound Library Drug Repurposing Compound Library Ion Channel Inhibitor Library Human Metabolite Library Inhibitor Library ReFRAME Related Library

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Keywords

Senicapoc 289656-45-7 Membrane transporter/Ion channel Potassium Channel KcsA inhibit ICA 17043 ICA17043 Inhibitor ICA-17043 inhibitor

 

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