VU0810464

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

VU0810464 是一种非 ureaG 蛋白门控内向整流钾通道（GIRK、Kir3）激活剂。

VU0810464 is a non-ureaG protein-gated inwardly-rectifying potassium channels (GIRK Kir3) activator.

VU0810464 (0, 0.1, 0.3, 1, 3, 10, 30 μM) produces a concentration‐dependent response curves of currents in SAN and HPC cells, in addition, VU0810464 is9‐fold higher potency for Kir3 channel activation in neurons as compared to SAN cells.

VU0810464 (intraperitoneal?injection;30 mg/kg,10 mg/kg; 30mg/kg; pre-treated 30 mins) produces a dose-dependent reduction of SIH response in Male C57BL/6J mice. To test if VU0810464 plays it role through Kir3 channel activation, VU0810464 (10 mg/kg) suppresses the SIH response in wild‐ type mice, but has no impact on Kcnj3?/? mice.VU0810464 (intraperitoneal?injection?; 30 mg/kg; 15, 30, 45, or 60 min post‐injection) displays a favourable distribution to the brain (Kp,uu = 0.83), has a improvement over ML297 (Kp,uu= 0.32).Clearance of VU0810464 is rapid,brain and plasma half-lives is 20 min in a PK study. Animal Model:Male C57BL/6J mice, Kcnj3?/? siblings female and maleC57BL/6J miceDosage:10 mg/kg; 30mg/kg Administration:Intraperitoneal?injection Result:Reduced stress‐induced hyperthermia (SIH), a physiological test of anxiolytic efficacy in wild mice, but had no impact in and Kcnj3 (Girk1) ?/?mice.

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Cell Cycle/DNA Damage

Potassium Channel

GIRK

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2126040-21-7

349.83

C18H21ClFN3O

>98% (HPLC)

DMSO:250 mg/mL (714.63 mM)

Cc1cc(NC(=O)Cc2ccc(F)c(Cl)c2)n(C2CCCCC2)n1

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(-20℃)

With Ice Pack

≥ 2 years