Cloperastine fendizoate inhibits the hERG K+ currents in a concentration-dependent manner with an IC50 value of 27 nM.
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产品名称 | Potassium Channel ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Tolbutamide | ✔ | 98% | |||||||||||||||||
Glimepiride |
++++
SUR1, IC50: 5.4 nM SUR2B, IC50: 7.3 nM |
97% | |||||||||||||||||
Dronedarone HCl | ✔ | 95% | |||||||||||||||||
Gliquidone |
++
Potassium channel, IC50: 27.2 nM |
99% | |||||||||||||||||
TRAM-34 |
+++
IKCa1 (KCa3.1), Kd: 20 nM |
98% | |||||||||||||||||
Glibenclamide | ✔ | 98% | |||||||||||||||||
Amiodarone HCl | ✔ | 97% | |||||||||||||||||
Gliclazide |
++
Potassium channel, IC50: 184 nM |
98% | |||||||||||||||||
Repaglinide | ✔ | 98% | |||||||||||||||||
Dofetilide | ✔ | 98% | |||||||||||||||||
Nateglinide | ✔ | 99% | |||||||||||||||||
Quinine HCl dihydrate | ✔ | 98% | |||||||||||||||||
ML133 HCl |
+
Kir2.1, IC50: 290 nM |
99% | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
描述 | Cloperastine disrupts hERG K+ currents in a concentration-dependent manner, displaying an IC50 value of 27±3 nM[1]. As an antitussive agent, cloperastine exhibits both antitussive and antiedemic activities and has the ability to relax bronchial musculature. It operates primarily through a central antitussive mechanism and has antihistaminic and papaverine-like activities, comparable to those of codeine but without the associated narcotic effects[2]. |
Animal study | In experiments with anesthetized guinea pigs, a therapeutic dose of cloperastine (1 mg/kg) was shown to prolong the QT interval and monophasic action potential (MAP) duration, though it did not affect the PR interval or QRS width[1].Cloperastine hydrochloride, when administered intraperitoneally, has relatively low acute toxicity in rats and mice. Additionally, when given orally in the form of cloperastine fendizoate, it demonstrates minimal toxicity, with the LD50 values for rats and mice exceeding 1000 mg/kg and 2000 mg/kg, respectively[2]. |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
1.54mL 0.31mL 0.15mL |
7.71mL 1.54mL 0.77mL |
15.43mL 3.09mL 1.54mL |
CAS号 | 85187-37-7 |
分子式 | C40H38ClNO5 |
分子量 | 648.19 |
SMILES Code | ClC1=CC=C(C(C2=CC=CC=C2)OCCN3CCCCC3)C=C1.O=C(O)C4=CC=CC=C4C(C5=CC(C6=CC=CC=C6)=C(O)C=C5)=O |
MDL No. | MFCD01661515 |
别名 | |
运输 | 蓝冰 |
InChI Key | PXZFKAKWSHBDCP-UHFFFAOYSA-N |
Pubchem ID | 163446 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Inert atmosphere, 2-8°C |
溶解方案 |
请根据您的动物给药指南选择适当的溶解方案。 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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