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VU0468554

Chemical Structure : VU0468554

CAS No.: 1448705-21-2

VU0468554 (VU 0468554)

Catalog No.: PC-72820Not For Human Use, Lab Use Only.

VU0468554 (VU 0468554) is a potent, selective inhibitor of GIRK channel with IC50 of 0.85 and 2.6 uM for GIRK1/GIRK4 and GIRK1/GIRK2 in cellular assays.

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Biological Activity

VU0468554 (VU 0468554) is a potent, selective inhibitor of GIRK channel with IC50 of 0.85 and 2.6 uM for GIRK1/GIRK4 and GIRK1/GIRK2 in cellular assays.
VU0468554 more effectively inhibits the cardiac GIRK channel than the neuronal GIRK channel, inhibits Gβγ-activated GIRK channels in noncompetitive and potentially uncompetitive fashion.
VU0468554 competitively inhibits GIRK-channel activation by ML297, a GIRK-channel activator.
In the isolated heart model, VU0468554 partially reversed carbachol-induced bradycardia in hearts from wild-type mice but not Girk4-/- mice.

Physicochemical Properties

M.Wt 334.423
Formula C20H22N4O
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 (3.34 mg/mL)

Chemical Name/SMILES

Urea, N-[3-(1-methylethyl)-1-phenyl-1H-pyrazol-5-yl]-N'-(3-methylphenyl)-

References

1. Allison Anderson, et al. Mol Pharmacol. 2021 Dec;100(6):540-547.

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