1. Membrane Transporter/Ion Channel
  2. Potassium Channel
  3. VU0134992

VU0134992 

Cat. No.: HY-122560
Handling Instructions

VU0134992 is the first subtype-preferring, orally active and selective Kir4.1 potassium channel pore blocker, with an IC50 of 0.97 µM. VU0134992 is 9-fold selective for homomeric Kir4.1 over Kir4.1/5.1 concatemeric channels (IC50=9 µM) at -120 mV.

For research use only. We do not sell to patients.

VU0134992 Chemical Structure

VU0134992 Chemical Structure

CAS No. : 755002-90-5

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Description

VU0134992 is the first subtype-preferring, orally active and selective Kir4.1 potassium channel pore blocker, with an IC50 of 0.97 µM. VU0134992 is 9-fold selective for homomeric Kir4.1 over Kir4.1/5.1 concatemeric channels (IC50=9 µM) at -120 mV[1].

IC50 & Target

IC50: 0.97 µM (Kir4.1)[1]

In Vitro

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[1]. The selectivity of VU0134992 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 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)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

VU0134992 (50-100 mg/kg; oral gavage) statistically significantly increased urinary Na+ as well as K+ excretion[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Sprague-Dawley rats (250-300 g)[1]
Dosage: 50 and 100 mg/kg
Administration: Oral gavage
Result: Statistically significantly increased urinary Na+ as well as K+ excretion
Molecular Weight

411.38

Formula

C₂₀H₃₁BrN₂O₂

CAS No.

755002-90-5

SMILES

O=C(NC1CC(C)(C)NC(C)(C)C1)COC2=CC=C(C(C)C)C=C2Br

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

VU0134992VU 0134992VU-0134992Potassium ChannelKcsAwhole-cellpatch-clampelectrophysiologydiuresisnatriuresiskaliuresishypertensionoralselectiveKir4.1Inhibitorinhibitorinhibit

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VU0134992
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