VU0810464|cas:2126040-21-7|西域试剂

VU0810464,99.33%

产品编号：Bellancom-127106| CAS NO：2126040-21-7| 分子式：C₁₈H₂₁ClFN₃O| 分子量：349.83

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货号	价格	库存与货期
Bellancom-127106	￥3500.00	杭州北京（现货）
Bellancom-127106	￥5500.00	杭州北京（现货）
Bellancom-127106	￥19500.00	杭州北京（现货）

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VU0810464

产品介绍

VU0810464 是有效的，选择性的非尿素蛋白门控的内向整流钾通道 (GIRK, Kir3) 激活剂。 VU0810464 对神经元 GIRK1/2 (EC₅₀=165 nM) 和 GIRK1/4 (EC₅₀=720 nM) 神经通道具有纳摩尔效价，并且具有脑部渗透性。

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 is 9‐fold higher potency for Kir3 channel activation in neurons as compared to SAN cells.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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 (K_p,uu = 0.83), has a improvement over ML297 (K_p,uu= 0.32). Clearance of VU0810464 is rapid,brain and plasma half-lives is 20 min in a PK study.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male C57BL/6J mice, Kcnj3^−/− siblings female and male C57BL/6J mice
Dosage:	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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male C57BL/6J mice, Kcnj3^−/− siblings female and male C57BL/6J mice
Dosage:	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.

性状

Solid

溶解性数据

In Vitro:

DMSO : ≥ 250 mg/mL (714.63 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.8585 mL	14.2927 mL	28.5853 mL
5 mM	0.5717 mL	2.8585 mL	5.7171 mL
10 mM	0.2859 mL	1.4293 mL	2.8585 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (5.95 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.95 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液