Name | 2,2-Bis(4-fluorophenyl)-2-phenylacetamide |
Synonyms | ICA17043 ICA-17043 Senicapoc ICA 17043 2,2-Bis(4-fluorophenyl)-2-phenylacetamide 2,2-bis(4-fluorophenyl)-2-phenyl-acetamide 4-Fluoro-A-(4-Fluorophenyl)-A-Phenyl-BenzeneacetaMide Benzeneacetamide, 4-fluoro-α-(4-fluorophenyl)-α-phenyl- Benzeneacetamide, 4-fluoro-a-(4-fluorophenyl)-a-phenyl- 4-Fluoro-alpha-(4-fluorophenyl)-alpha-phenylbenzeneacetamide |
CAS | 289656-45-7 |
InChI | InChI=1/C20H15F2NO/c21-17-10-6-15(7-11-17)20(19(23)24,14-4-2-1-3-5-14)16-8-12-18(22)13-9-16/h1-13H,(H2,23,24) |
Molecular Formula | C20H15F2NO |
Molar Mass | 323.34 |
Density | 1.250±0.06 g/cm3(Predicted) |
Melting Point | 180-181 °C(Solv: hexane (110-54-3); dichloromethane (75-09-2)) |
Boling Point | 460.7±45.0 °C(Predicted) |
Flash Point | 232.4°C |
Vapor Presure | 1.14E-08mmHg at 25°C |
pKa | 15.41±0.50(Predicted) |
Storage Condition | Sealed in dry,Store in freezer, under -20°C |
Refractive Index | 1.594 |
Use | Senicapoc(ICA17043) is a Gardos channel blocker, which can inhibit calcium ion-induced rubidium flow of human red blood cells (RBC) with an IC50 of 11 nM and dehydration of red blood cells (RBC) with an IC50 of 30 nM. |
In vitro study | ICA-17043 is shown to block the Gardos channel of mouse (C57 Black) RBCs with an IC 50 of 50±6 nM. ICA-17043 blocks this increase in cellular hemoglobin concentration in human RBCs in a concentration-dependent fashion. |
In vivo study | 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. 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. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 3.093 ml | 15.463 ml | 30.926 ml |
5 mM | 0.619 ml | 3.093 ml | 6.185 ml |
10 mM | 0.309 ml | 1.546 ml | 3.093 ml |
5 mM | 0.062 ml | 0.309 ml | 0.619 ml |
biological activity | Senicapoc (ICA-17043) is an effective and selective Gardos channel (Ca2 + activated K channel; KCa3.1) blocker with IC50 of 11 nM. Senicapoc blocking Ca2 +-induced rubidium flux from human erythrocytes, the IC50 value is 11 nM, and the IC50 for inhibiting erythrocyte dehydration is 30 nM. |
target | IC50: 11 nM (Gardos channel) |