4-氟-A-(4-氟苯基)-A-苯基-苯甲酰胺

4-氟-A-(4-氟苯基)-A-苯基-苯甲酰胺化学性质

熔点 :180-181 °C(Solv: hexane (110-54-3); dichloromethane (75-09-2))
沸点 :460.7±45.0 °C(Predicted)
密度 :1.250±0.06 g/cm3(Predicted)
储存条件 :Sealed in dry,Store in freezer, under -20°C
溶解度 :DMSO : 50 mg/mL (154.64 mM; Need ultrasonic)
形态 :Powder
酸度系数(pKa) :15.41±0.50(Predicted)
颜色 :White to yellow
InChI :InChI=1S/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)
InChIKey :SCTZUZTYRMOMKT-UHFFFAOYSA-N
SMILES :C(C1C=CC=CC=1)(C1C=CC(F)=CC=1)(C1C=CC(F)=CC=1)C(=O)N

4-氟-A-(4-氟苯基)-A-苯基-苯甲酰胺性质、用途与生产工艺

生物活性 Senicapoc (ICA-17043) 是有效，选择性的 Gardos 通道 (Ca2+ 激活的 K+ 通道; KCa3.1) 阻断剂，IC50 为 11 nM。Senicapoc 阻断来自人红细胞的 Ca2+ 诱导的铷通量，IC50 值为 11 nM，抑制红细胞脱水的 IC50 为 30 nM。
靶点

IC50: 11 nM (Gardos channel)
体外研究

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.
体内研究

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.

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