货号:A1219196
同义名:
A2764 (hydrochloride); A2764 dihydrochloride
A2764 dihydrochloride is a selective inhibitor of TRESK (KCNK18) with an IC50 value of 11.8 μM. A2764 can inhibit TRESK in native cells, leading to cell depolarization and increased excitability.
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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 | A2764 2HCl is a highly selective inhibitor of TRESK (TWIK-related spinal cord K+ channel, K2P18.1), which has moderate inhibitory effects on TREK-1 and TALK-1. A2764 dihydrochloride is more sensitive to the activated mTRESK channels (IC50=6.8 μM) than the basal current. A2764 dihydrochloride can lead to cell depolarization and increased excitability in native cells, it has the potential for probing the role of TRESK channel in migraine and nociception. The degree of inhibition by 100 µM A2764 (77.8% ± 3.5%, n = 6) was larger in the activated state of TRESK (i.e., after calcineurin-dependent stimulation) than in the resting state of the channel (42.8% ± 11.5% inhibition, n = 7). A2764 (100 µM) shows an improved inhibitory potency for activated channel. The subsequent application of A2764 strongly inhibits the current (77.8±3.5%)[1]. |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.84mL 0.57mL 0.28mL |
14.22mL 2.84mL 1.42mL |
28.43mL 5.69mL 2.84mL |
CAS号 | 861038-72-4 |
分子式 | C15H21Cl3N2O |
分子量 | 351.7 |
SMILES Code | ClC1=C2C=CC=NC2=C(OCCN(CC)CC)C=C1.[H]Cl.[H]Cl |
MDL No. | MFCD32667019 |
别名 | A2764 (hydrochloride); A2764 dihydrochloride |
运输 | 蓝冰 |
InChI Key | ZVRDPULCSHGKBD-UHFFFAOYSA-N |
Pubchem ID | 146013302 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Sealed in dry,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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