VU0134992

SKU: orb1298990

Description

VU0134992 is a selective Kir4.1 potassium channel inhibitor with a half-maximal inhibitory concentration (IC50) of 0.97 µM. This tool compound is used in neuroscience research to study astrocyte function and potassium buffering in both in vitro cellular models and in vivo experimental systems.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 755002-90-5
• MW: 411.38
• Purity: 99.86%
• Formula: C₂₀H₃₁BrN₂O₂
• SMILES: N(C(COC1=C(Br)C=C(C(C)C)C=C1)=O)C2CC(C)(C)NC(C)(C)C2
• Target: Potassium Channel
• Solubility: DMSO:60 mg/mL (145.85 mM)

Bioactivity

• Target IC50:
  KIR4.1:0.97 µM
• In Vivo:
  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.
• In Vitro:
  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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

hypertension, Inhibitor, electrophysiology, kaliuresis, inhibit, KcsA, Kir4.1, patch-clamp, natriuresis, oral, diuresis, whole-cell, PotassiumChannel, Potassium Channel, selective, VU0134992, VU-0134992, VU 0134992

Compound Identifiers

PubChem CID

1319582