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Senicapoc  ≥98%

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包装规格：10mg 50mg 100mg in glass bottle
溶解性：溶于DMSO(50mg/ml 超声)
产品描述：基本信息 产品编号： S10974 产品名称： Senicapoc CAS: 289656-45-7   储存条件 粉末 -20℃ 四年     分子式： C20H15F2NO 溶于液体 -80℃ 6个月 分子量： 323.34 -20℃ 1个月 化学名：  Benzeneacetamide,4-fluoro-alpha-(4-fluorophenyl)-alpha-phenyl- Solubility (25°C)：   体外:   DMSO 65mg/mL Ethanol 6mg/mL Water Insoluble 体内(现配现用):   ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 3.0927mL 15.4636mL 30.9272mL 5mM 0.6185mL 3.0927mL 6.1854mL 10mM 0.3093mL 1.5464mL 3.0927mL   生物活性 产品描述 一种有效，选择性的Gardos通道(Ca2+激活的K+通道;KCa3.1)阻断剂。 靶点 IC50:11nM (Gardos channel)   体外研究 ICA-17043 is shown to block the Gardos channel of mouse (C57 Black) RBCs with an IC50 of 50±6nM.ICA-17043 blocks this increase in cellular hemoglobin concentration in human RBCs in a concentration-dependent fashion. 体内研究 ICA-17043 (10mg/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 (10mg/kg,twice a day) induces a significant increase in Hct after 11 days of dosing in the SAD mouse.Senicapoc (30mg/kg,p.o.) reduces airway hyperresponsiveness,eosinophil numbers in bronchoalveolar lavage taken 48 hours post-allergen challenge,and vascular remodelling in the sheep.   推荐实验方法(仅供参考) 细胞实验:   The whole blood is initially diluted 1:1 with Modified Flux Buffer (MFB),consisting of 140mM NaCl,5mM KCl,10mM Tris (tris(hydroxymethyl)aminomethane),0.1mM EGTA (ethyleneglycoltetraacetic acid) (pH=7.4).The blood is centrifuged at 1000 rpm,and the pellet comprised primarily of RBCs is washed 3 times with MFB.The cells are then loaded with 86Rb+ by incubating the washed cells with 86Rb+at a final concentration of 0.185 MBq/mL (5μCi/mL) in MFB for at least 3 hours at 37℃.After loading with 86Rb+,the RBCs are washed 3 times with chilled MFB.The cells are then incubated for 10 minutes with test compound (senicapoc) at concentrations that ranged from 1nM to 10 000nM.Efflux of 86Rb+is initiated by raising intracellular calcium levels in the RBCs with the addition of CaCl2 and A23187 (a calcium ionophore) to final concentrations of 2mM and 5μM,respectively. After 10 minutes of incubation at room temperature,the RBCs are pelleted in a microcentrifuge, and the supernatant is removed and counted in a Wallac MicroBeta liquid scintillation counter.   动物实验:   Transgenic Hbbsingle/single SAD1 (SAD) female and male mice between 3 and 6 months of age,weighing 25 to 30g,are used for this study. The SAD mice are divided into 2 groups,and either vehicle (n=6) or senicapoc (10mg/kg) (n=6) is administered orally by gavage twice daily.C57B6/2J mice are used as controls (wild-type mice).Hematologic parameters are evaluated at baseline and after 11 and 21 days of therapy.Blood sampling and vehicle administration have previously been shown not to affect the blood parameters measured in this study.
保存条件：-20℃

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