An inhibitor of heteromeric Kir4.1/5.1 channels
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VU6036720 (hydrochloride)

Item No. 40286

Technical Information
Formal Name
3-chloro-N-[2-[(2S)-4-(2-cyanophenyl)-2-methyl-1-piperazinyl]ethyl]-4-fluoro-benzenesulfonamide, monohydrochloride
Molecular Formula
C20H22ClFN4O2S • HCl
Formula Weight
Purity
≥95%
Formulation
A solid
Acetonitrile: Slightly SolubleDMSO: SolubleWater: Slightly Soluble
SMILES
O=S(C1=CC=C(F)C(Cl)=C1)(NCCN2CCN(C3=CC=CC=C3C#N)C[C@@H]2C)=O.Cl
InChi Code
InChI=1S/C20H22ClFN4O2S.ClH/c1-15-14-26(20-5-3-2-4-16(20)13-23)11-10-25(15)9-8-24-29(27,28)17-6-7-19(22)18(21)12-17;/h2-7,12,15,24H,8-11,14H2,1H3;1H/t15-;/m0./s1
InChi Key
ZRUTWJFQZLMEBJ-RSAXXLAASA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    VU6036720 is an inhibitor of heteromeric inward-rectifier potassium channels (Kir) composed of Kir4.1 and Kir5.1 subunits (IC50 = 0.24 µM).1 It is selective for Kir4.1/5.1 channels over a variety of homomeric Kir channels, including Kir4.1 (IC50 = >10 µM), as well as heteromeric Kir3.1/3.2, Kir3.1/3.4, Kir6.2/SUR1, and Kir6.1/SUR2b channels at 30 µM but does inhibit the voltage-gated potassium channel Kv11.1, also known as human ether-a-go-go (hERG; IC50 = 6.4 µM). VU6036720 (30 and 100 mg/kg) does not inhibit diuresis in mice due to low oral bioavailability and high hepatic clearance.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. McClenahan, S.J., Kent, C.N., Kharade, S.V., et alVU6036720: The first potent and selective in vitro inhibitor of heteromeric Kir4.1/5.1 inward rectifier potassium channels. Mol. Pharmacol. 101(5), 357-370 (2022).