Cas No.: | 289656-45-7 |
Chemical Name: | ICA-17043;ICA 17043;ICA17043 |
Synonyms: | ICA-17043;ICA 17043;ICA17043 |
SMILES: | O=C(C(C1=CC=CC=C1)(C2=CC=C(C=C2)F)C3=CC=C(F)C=C3)N |
Formula: | C20H15F2NO |
M.Wt: | 323.336 |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
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. |
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]. |
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]. |