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VU6036720

Chemical Structure : VU6036720

CAS No.: 3026597-12-3

VU6036720 (VU 6036720)

Catalog No.: PC-72872Not For Human Use, Lab Use Only.

VU6036720 (VU 6036720) is the first potent, selective inhibitor of heteromeric Kir4.1/Kir5.1 (KCNJ10/KCNJ16) with IC50 of 0.24 uM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

    Biological Activity

    VU6036720 (VU 6036720) is the first potent, selective inhibitor of heteromeric Kir4.1/Kir5.1 (KCNJ10/KCNJ16) with IC50 of 0.24 uM.
    VU6036720 displays >30-fold selective for Kir4.1/5.1 over homomeric Kir4.1 channels, Kir1.1, Kir2.1, Kir2.2, Kir2.3, Kir4.2, Kir6.2/SUR1, Kir6.1/SUR2b and Kir7.1.
    VU6036720 inhibits Kir4.1/5.1 activity through a reduction of channel open-state probability and single-channel current amplitude, does not induce diuresis in vivo.
    VU6036720 showwd an IC50 in 3 uM in Tl+ flux assays, approximately 7-times more potent at inhibiting Kir4.1/5.1 than fluoxetine and amitriptyline.
    VU6036720 represents the current state-of-the-art Kir4.1/5.1 inhibitor that should be useful for probing the functions of Kir4.1/5.1 in vitro and ex vivo.

    Physicochemical Properties

    M.Wt 436.93
    Formula C20H22ClFN4O2S
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20°C 12 Months; 4°C 6 Months
    In Solvent
    -80°C 6 Months; -20°C 6 Months
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

    (S)-3-chloro-N-(2-(4-(2-cyanophenyl)-2-methylpiperazin-1-yl)ethyl)-4-fluorobenzenesulfonamide

    References

    1. McClenahan SJ, et al. Mol Pharmacol. 2022 Mar 3:MOLPHARM-AR-2021-000464.

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