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VU0134992 HCl

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Chemical Structure| 1052515-91-9 同义名 : VU0134992 hydrochloride
CAS号 : 1052515-91-9
货号 : A1324873
分子式 : C20H32BrClN2O2
纯度 : 98%+
分子量 : 447.837
MDL号 : MFCD05985784
存储条件：

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
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：
生物活性
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].
实验方案
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
参考文献

[1]Kharade SV, et al. Discovery, Characterization, and Effects on Renal Fluid and Electrolyte Excretion of the Kir4.1 Potassium Channel Pore Blocker, VU0134992. Mol Pharmacol. 2018 Aug;94(2):926-937.