VU6036720 | Kir4.1/Kir5.1 inhibitor | Probechem Biochemicals

Chemical Structure : VU6036720

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VU6036720 (VU 6036720)

货号: 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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生物&药学活性

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.

物理化学性质&存储条件

分子量	436.93
分子式	C20H22ClFN4O2S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(S)-3-chloro-N-(2-(4-(2-cyanophenyl)-2-methylpiperazin-1-yl)ethyl)-4-fluorobenzenesulfonamide

参考文献

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

VU6036720 (VU 6036720)

生物&药学活性

物理化学性质&存储条件

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VU6036720 (VU 6036720)

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物理化学性质&存储条件

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