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Home - Products - Cell Cycle/DNA Damage - Potassium Channel - VU 0134992

VU 0134992

CAS No. 755002-90-5

VU 0134992( —— )

Catalog No. M21660 CAS No. 755002-90-5

VU0134992 is an Kir4.1 blocker with an IC50 value of 0.97 μM.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    VU 0134992
  • Note
    Research use only, not for human use.
  • Brief Description
    VU0134992 is an Kir4.1 blocker with an IC50 value of 0.97 μM.
  • Description
    VU0134992 is an Kir4.1 blocker with an IC50 value of 0.97 μM.
  • 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.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).
  • In Vivo
    VU0134992 (50-100 mg/kg; oral gavage) statistically significantly increased urinary Na+ as well as K+ excretion. Animal Model:Male Sprague-Dawley rats (250-300 g)Dosage:50 and 100 mg/kg Administration:Oral gavage Result:Statistically significantly increased urinary Na+ as well as K+ excretion
  • Synonyms
    ——
  • Pathway
    Cell Cycle/DNA Damage
  • Target
    Potassium Channel
  • Recptor
    Kir4.1
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    755002-90-5
  • Formula Weight
    411.38
  • Molecular Formula
    C20H31BrN2O2
  • Purity
    >98% (HPLC)
  • Solubility
    ——
  • SMILES
    CC(C)c1ccc(OCC(=O)NC2CC(C)(C)NC(C)(C)C2)c(Br)c1
  • Chemical Name
    2-(2-Bromo-4-isopropylphenoxy)-N-(2266-tetramethylpiperidin-4-yl)acetamide

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

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.
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