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Senicapoc (ICA-17043) 是有效的,选择性的Gardos 通道 (Ca2+激活的 K+通道;KCa3.1) 阻断剂,IC50为 11 nM。Senicapoc 阻断人红细胞的 Ca2+诱导的铷通量,IC50为 11 nM, 抑制红细胞脱水的IC50为 30 nM。
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Senicapoc (ICA-17043) 是有效的,选择性的Gardos 通道 (Ca2+激活的 K+通道;KCa3.1) 阻断剂,IC50为 11 nM。Senicapoc 阻断人红细胞的 Ca2+诱导的铷通量,IC50为 11 nM, 抑制红细胞脱水的IC50为 30 nM。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 119 | 现货 | |
2 mg | ¥ 168 | 现货 | |
5 mg | ¥ 285 | 现货 | |
10 mg | ¥ 415 | 现货 | |
25 mg | ¥ 690 | 现货 | |
50 mg | ¥ 987 | 现货 | |
100 mg | ¥ 1,390 | 现货 | |
200 mg | ¥ 1,980 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 297 | 现货 |
产品描述 | Senicapoc (ICA-17043) is a potent inhibitor of the Gardos channel and ameliorates RBC dehydration in the SAD mouse. Senicapoc blocked Ca2+-induced rubidium flux from human RBCs with an IC50 value of 11 ± 2 nM (CLT IC50 = 100 ± 12 nM) and inhibited RBC dehydration with an IC50 of 30 ± 20 nM. Senicapoc is in treatment of Sickle Cell Disease and Sickle Cell Anemia |
靶点活性 | RBC:30 ± 20 nM, RBCs (human):11 ± 2 nM |
体外活性 | ICA-17043 能够阻断小鼠(C57 Black)红细胞的 Gardos 通道,其 IC50 为 50±6 nM。ICA-17043 以浓度依赖的方式阻止了人类红细胞内血红蛋白浓度的增加[1]。 |
体内活性 | ICA-17043(10 mg/kg,口服)给药后,在第11天和第21天测量的Gardos通道活性显著降低,并且伴随红细胞K+含量的相应增加,而Na+含量未发生变化。ICA-17043(10 mg/kg,每天两次)在连续给药11天后,显著增加SAD小鼠的Hct水平[1]。Senicapoc(30 mg/kg,口服)在过敏原挑战后48小时取材的支气管肺泡灌洗液中减少嗜酸粒细胞数量,减轻气道高反应性和羊只的血管重塑[2]。 |
细胞实验 | Senicapoc is dissolved in DMSO or 100% ethanol. The whole blood is initially diluted 1:1 with Modified Flux Buffer (MFB), consisting of 140 mM NaCl, 5 mM KCl, 10 mM Tris (tris(hydroxymethyl)aminomethane), 0.1 mM 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 (5 μCi/mL) in MFB for at least 3 hours at 37°C. 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 1 nM to 10?000 nM. 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 2 mM and 5 μM, 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. |
别名 | 塞尼卡泊, ICA-17043 |
分子量 | 323.34 |
分子式 | C20H15F2NO |
CAS No. | 289656-45-7 |
Smiles | NC(=O)C(c1ccccc1)(c1ccc(F)cc1)c1ccc(F)cc1 |
密度 | 1.250 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 50 mg/mL (154.64 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
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