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[1].

Product Specifications

CAS Number

[1052515-91-9]

UNSPSC

12352005

Hazard Statement

H302-H315-H319-H335

Target

Potassium Channel

Type

Reference compound

Related Pathways

Membrane Transporter/Ion Channel

Applications

COVID-19-immunoregulation

Field of Research

Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/vu0134992-hydrochloride.html

Purity

98.49

Solubility

DMSO : 250 mg/mL (ultrasonic) |H2O : 2.27 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O=C(NC1CC(C)(C)NC(C)(C)C1)COC2=CC=C(C(C)C)C=C2Br.[H]Cl

Molecular Formula

C20H32BrClN2O2

Molecular Weight

447.84

Precautions

P261-P264-P270-P271-P280-P302+P352-P304+P340-P305+P351+P338-P330-P362+P364-P403+P233-P405-P501

References & Citations

[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.