VU0134992

VU0134992CAS号: 755002-90-5分子式: C20H31BrN2O分子量: 411.38描述纯度储存/保存方法In vitro(体外研究)In vivo(体内研究)

产品描述
描述
VU0134992 is an Kir4.1 blocker with an IC50 value of 0.97 µM 
纯度
98%
储存/保存方法
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
生物活性
In vitro(体外研究)
VU0134992 inhibits Kir4.1 with an IC50 value of 0.97 µM and is 9-fold selective for homomeric Kir4.1 over Kir4.1/5.1 concatemeric channels (IC50 = 9 µM) at -120 mV. In thallium (Tl+) flux assays, VU0134992 is greater than 30-fold selective for Kir4.1 over Kir1.1, Kir2.1, and Kir2.2; is weakly active toward Kir2.3, Kir6.2/SUR1, and Kir7.1; and is equally active toward Kir3.1/3.2, Kir3.1/3.4, and Kir4.2.
In vivo(体内研究)
VU0134992 displayed a large free unbound fraction (fu) in rat plasma (fu = 0.213). Consistent with the known role of Kir4.1 in renal function, oral dosing of VU0134992 led to a dose-dependent diuresis, natriuresis, and kaliuresis in rats.

分子结构图

VU0134992