VU0134992 hydrochloride

Chemical Structure : VU0134992 hydrochloride

CAS No.: 1052515-91-9

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货号: PC-23611Not For Human Use, Lab Use Only.

VU0134992 hydrochloride(VU 0134992) is a potent, selective blocker of the inward rectifier potassium channel Kir4.1 (KCNJ10) with IC50 of 0.97 uM in whole-cell patch clamp electrophysiology assays.

规格	价格	库存
5 mg	￥680	In stock
10 mg	￥980	In stock
50 mg	￥2580	In stock
100 mg	￥4280	In stock
250 mg		Get quote

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生物&药学活性

VU0134992 hydrochloride(VU 0134992) is a potent, selective blocker of the inward rectifier potassium channel Kir4.1 (KCNJ10) with IC50 of 0.97 uM in whole-cell patch clamp electrophysiology assays.
VU0134992 displays 9-fold selectivity for homomeric Kir4.1 over Kir4.1/5.1 concatemeric channels (IC50=9 uM) at -120 mV.
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 Tl+ flux assays.
VU0134992 causes dose-dependent diuresis, natriuresis, and kaliuresis in rats after oral treatment.
VU0134992 represents the first in vivo-active tool compound for probing the therapeutic potential of Kir4.1 as a novel diuretic target for the treatment of hypertension.

物理化学性质&存储条件

分子量	447.84
分子式	C20H32BrClN2O2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	2-(2-Bromo-4-isopropylphenoxy)-N-(2,2,6,6-tetramethylpiperidin-4-yl)acetamide hydrochloride

参考文献

1. Kharade SV, et al. Mol Pharmacol. 2018 Jun 12. pii: mol.118.112359.