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289656-45-7

中文名稱 4-氟-A-(4-氟苯基)-A-苯基-苯甲酰胺
英文名稱 2,2-bis(4-fluorophenyl)-2-phenyl-acetamide
CAS 289656-45-7
分子式 C20H15F2NO
分子量 323.34
MOL 文件 289656-45-7.mol
289656-45-7 結(jié)構(gòu)式 289656-45-7 結(jié)構(gòu)式

基本信息

中文別名
塞尼卡泊
2,2-雙(4-氟苯)-2-苯乙酰胺
2,2-雙(4-氟苯基)-2-苯乙酰胺
4-氟-A-(4-氟苯基)-A-苯基-苯甲酰胺
4-氟-ALPHA-(4-氟苯基)-ALPHA-苯基苯乙酰胺
英文別名
Senicapoc
ICA 17043
ICA-17043
ICA 17043
ICA17043
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
所屬類別
生物化工:激動劑抑制劑

物理化學(xué)性質(zhì)

熔點180-181 °C(Solv: hexane (110-54-3); dichloromethane (75-09-2))
沸點460.7±45.0 °C(Predicted)
密度1.250±0.06 g/cm3(Predicted)
儲存條件Sealed in dry,Store in freezer, under -20°C
溶解度DMSO : 50 mg/mL (154.64 mM; Need ultrasonic)
酸度系數(shù)(pKa)15.41±0.50(Predicted)
形態(tài)粉末
顏色White to yellow
InChIInChI=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)
InChIKeySCTZUZTYRMOMKT-UHFFFAOYSA-N
SMILESC(C1C=CC=CC=1)(C1C=CC(F)=CC=1)(C1C=CC(F)=CC=1)C(=O)N

常見問題列表

生物活性
Senicapoc (ICA-17043) 是有效,選擇性的 Gardos 通道 (Ca2+ 激活的 K+ 通道; KCa3.1) 阻斷劑,IC50 為 11 nM。Senicapoc 阻斷來自人紅細胞的 Ca2+ 誘導(dǎo)的銣通量,IC50 值為 11 nM, 抑制紅細胞脫水的 IC50 為 30 nM。
靶點

IC50: 11 nM (Gardos channel)

體外研究

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.

體內(nèi)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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111982-45-7 18063-03-1