产品
编 号：F563737
分子式：C18H21ClFN3O
分子量：349.83
分子式：C18H21ClFN3O
分子量：349.83
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
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1mg
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5mg
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10mg
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25mg
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50mg
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结构图
CAS No: 2126040-21-7
产品详情
生物活性：
VU0810464 is a potent and selective non-ureaG protein-gated inwardly-rectifying potassium channels (GIRK, Kir3) activator. VU0810464 displays nanomolar potency for neuronal (EC50=165 nM) and GIRK1/4 (EC50=720 nM) channels with improved brain penetration.
体内研究：
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 mice
Dosage:10 mg/kg; 30mg/kg
Administration:Intraperitoneal?injection
Result:Reduced stress‐induced hyperthermia (SIH), a physiological test ofanxiolytic efficacy in wild mice, but had no impact in and Kcnj3 (Girk1) ?/?mice.
体外研究：
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 is a potent and selective non-ureaG protein-gated inwardly-rectifying potassium channels (GIRK, Kir3) activator. VU0810464 displays nanomolar potency for neuronal (EC50=165 nM) and GIRK1/4 (EC50=720 nM) channels with improved brain penetration.
体内研究：
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 mice
Dosage:10 mg/kg; 30mg/kg
Administration:Intraperitoneal?injection
Result:Reduced stress‐induced hyperthermia (SIH), a physiological test ofanxiolytic efficacy in wild mice, but had no impact in and Kcnj3 (Girk1) ?/?mice.
体外研究：
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.
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