货号:A1324873 同义名: VU0134992 hydrochloride
VU0134992 hydrochloride is the first subtype-preferring, orally active and selective Kir4.1 potassium channel pore blocker, with an IC50 of 0.97 µM. VU0134992 hydrochloride is 9-fold selective for homomeric Kir4.1 over Kir4.1/5.1 concatemeric channels (IC50=9 µM) at -120 mV.
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产品名称 | Potassium Channel ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Tolbutamide | ✔ | 98% | |||||||||||||||||
Glimepiride |
++++
SUR2B, IC50: 7.3 nM SUR1, IC50: 5.4 nM |
97% | |||||||||||||||||
Dronedarone Hydrochloride | ✔ | 95% | |||||||||||||||||
Gliquidone |
++
Potassium channel, IC50: 27.2 nM |
98% | |||||||||||||||||
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 hydrochloride dihydrate | ✔ | 98% | |||||||||||||||||
ML133 HCl |
+
Kir2.1, IC50: 290 nM |
97% | |||||||||||||||||
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 | VU0134992 HCl is the first subtype-preferring, orally active and selective Kir4.1 potassium channel pore blocker with an IC50 of 0.97 µM. At -120 mV, VU0134992 HCl is 9 times more selective for homologous Kir4.1 than the Kir4.1/5.1 merged channel (IC50=9 µM)[1].VU0134992 HCl is more than 30-fold selective for Kir4.1 over Kir1.1, Kir2.1, and Kir2.2, less active for Kir2.3, Kir6.2/SUR1, and Kir7.1, and equally active for Kir3.1/3.2, Kir3.1/3.4, and Kir4.2[1]. |
Animal study | VU0134992 HCl significantly increased urinary excretion of Na+ and K+ in rats when administered by gavage at doses of 50-100 mg/kg[1]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.23mL 0.45mL 0.22mL |
11.16mL 2.23mL 1.12mL |
22.33mL 4.47mL 2.23mL |
CAS号 | 1052515-91-9 |
分子式 | C20H32BrClN2O2 |
分子量 | 447.837 |
别名 | VU0134992 hydrochloride |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Inert atmosphere,Room Temperature |
溶解度 |
DMSO: 250 mg/mL(558.24 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO H2O: 2 mg/mL(4.47 mM),配合低频超声,并水浴加热至45℃助溶 |
动物实验配方 |