VU0134992 hydrochloride 是第一个亚型偏好的，具有口服活性和选择性的内向整流钾通道 Kir4.1 阻滞剂，IC₅₀ 值为 0.97 μM。VU0134992 hydrochloride 在 -120 mV 时，对同分 Kir4.1 比 Kir4.1/5.1 共分通道 (IC₅₀=9 μM) 高出 9 倍的选择性。

VU0134992 hydrochloride is the first subtype-preferring, orally active and selective Kir4.1 potassium channel pore blocker, with an IC 50 of 0.97 μM. VU0134992 hydrochloride is 9-fold selective for homomeric Kir4.1 over Kir4.1/5.1 concatemeric channels (IC 50 =9 μM) at -120 mV.

Solid

VU0134992 hydrochloride 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.The selectivity of VU0134992 hydrochloride for Kir4.1 versus nine other members of the Kir channel family was evaluated at concentrations ranging from 0.3 nM to 30 μM in 11-point CRC experiments, using established Tl+ flux assays. VU0134992 hydrochloride inhibits Kir3.1/Kir3.2 (92% inhibition at 30 μM, IC50=2.5 μM), Kir3.1/Kir3.4 (92% inhibition at 30 μM, IC50=3.1 μM), and Kir4.2 (100% inhibition at 30 μM, IC50=8.1 μM) with approximately the same efficacy and potency that VU0134992 inhibits Kir4.1 (100% at 30 μM, IC50=5.2 μM). has not independently confirme

VU0134992 hydrochloride (50-100 mg/kg; oral gavage) statistically significantly increased urinary Na as well as K excretion. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male Sprag

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

[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.

In Vitro: DMSO : 250 mg/mL (558.24 mM; Need ultrasonic)H₂O : 2.27 mg/mL (5.07 mM; ultrasonic and warming and heat to 60°C)配制储备液