Product Data SheetProduct Name:CAS No.: Cat.No.:Cat. No.:MWt:Formula:Purity :Senicapoc289656-45-7HY-50694HY50694323.34C20H15F2NO>98%Solubility:DMSOMechanisms: Pathways:Membrane Tranporter/Ion Channel; Target:Potassiun Channel Biological Activity:Senicapoc(ICA17043) is a potent and selective Gardos channel blocker; blocked Ca(2+)-inducedSi(ICA17043)idliGdhlblkblkdC(2)iddrubidium flux from human RBCs/ inhibited RBC dehydration with IC50s of 11 nM/30 nM,respectively. IC50 value: 11/30 nM [1] Target: Gardos channel in vitro: ICA-17043 blocked Ca(2+)-induced rubidium flux from human RBCs with an IC(50) value of11 +/- 2 nM (CLT IC(50) = 100 +/- 12 nM) and inhibited RBC dehydration with an IC(50) of 30 +/- 20nM [1]. invivo:Inatransgenicmousemodelofsicklecelldisease(SAD)treatmentwithICA-17043in vivo: In a transgenic mouse model of sickle cell disease (SAD), treatment with ICA17043 (10(10mg/kg orally, twice a day) for 21 days showed a marked and constant inhibition of the Gardoschannel activity (with an average inhibition of 90% +/- 27%, P <.005), an increase in RBC K(+)content (from 392 +/- 19.9 to 479.2 +/- 40 mmol/kg hemoglobin [Hb], P <.005), a significant increaseReferences:[1]. Stocker JW, et al. ICA-17043, a novel Gardos channel blocker, prevents sickled red blood celldehydration in vitro and in vivo in SAD mice. Blood. 2003 Mar 15;101(6):2412-8. [2]. Ataga KI, et al. Senicapoc (ICA-17043): a potential therapy for the prevention and treatment ofhemolysis-associated complications in sickle cell anemia. Expert Opin Investig Drugs. 2009OFeb;18(2):231-9. [3]. Van Der Velden J, et al. K(Ca)3.1 channel-blockade attenuates airway pathophysiology in asheep model of chronic asthma. PLoS One. 2013 Jun 24;8(6):e66886. Caution: Not fully tested. For research purposes onlyMedchemexpress LLCwww.medchemexpress.com 18 Wilkinson Way, Princeton, NJ 08540,USAess.com Web: www.medchemexpress.comEmail: info@medchemexpr