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

VU0134992 hydrochloride 

Cat. No.: HY-122560A Purity: 99.57%
Handling Instructions

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.

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

VU0134992 hydrochloride Chemical Structure

VU0134992 hydrochloride Chemical Structure

CAS No. : 1052515-91-9

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Based on 1 publication(s) in Google Scholar

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Description

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].

In Vitro

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[1]. 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)[1].

In Vivo

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

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

447.84

Formula

C₂₀H₃₂BrClN₂O₂

CAS No.

1052515-91-9

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (558.24 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2329 mL 11.1647 mL 22.3294 mL
5 mM 0.4466 mL 2.2329 mL 4.4659 mL
10 mM 0.2233 mL 1.1165 mL 2.2329 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.64 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (4.64 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.64 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

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

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VU0134992 hydrochloride
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