VU0134992 hydrochloride|cas:1052515-91-9|西域试剂

VU0134992 hydrochloride,98.34%

产品编号：Bellancom-122560A| CAS NO：1052515-91-9| 分子式：C₂₀H₃₂BrClN₂O₂| 分子量：447.84

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货号	价格	库存与货期
Bellancom-122560A	￥700.00	杭州北京（现货）
Bellancom-122560A	￥1250.00	杭州北京（现货）
Bellancom-122560A	￥3800.00	杭州北京（现货）
Bellancom-122560A	￥6500.00	杭州北京（现货）

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VU0134992 hydrochloride

产品介绍

VU0134992 hydrochloride 是第一个亚型偏好的，具有口服活性和选择性的内向整流钾通道 Kir4.1 阻滞剂，IC₅₀ 值为 0.97 μM。VU0134992 hydrochloride 在 -120 mV 时，对同分 Kir4.1 比 Kir4.1/5.1 共分通道 (IC₅₀=9 μM) 高出 9 倍的选择性。

生物活性

VU0134992 hydrochloride is the first subtype-preferring, orally active and selective Kir4.1 potassium channel pore blocker, with an IC₅₀ of 0.97 µM. VU0134992 hydrochloride is 9-fold selective for homomeric Kir4.1 over Kir4.1/5.1 concatemeric channels (IC₅₀=9 µM) at -120 mV.

体外研究

VU0134992 hydrochloride is greater than 30-fold selective for Kir4.1 over Kir1.1, Kir2.1, and Kir2.2, is weakly active toward Kir2.3, Kir6.2/SUR1, and Kir7.1, and is equally active toward Kir3.1/3.2, Kir3.1/3.4, and Kir4.2. The selectivity of VU0134992 hydrochloride for Kir4.1 versus nine other members of the Kir channel family was evaluated at concentrations ranging from 0.3 nM to 30 µM in 11-point CRC experiments, using established Tl+ flux assays. VU0134992 hydrochloride inhibits Kir3.1/Kir3.2 (92% inhibition at 30 µM, IC₅₀=2.5 µM), Kir3.1/Kir3.4 (92% inhibition at 30 µM, IC₅₀=3.1 µM), and Kir4.2 (100% inhibition at 30 µM, IC₅₀=8.1 µM) with approximately the same efficacy and potency that VU0134992 inhibits Kir4.1 (100% at 30 µM, IC₅₀=5.2 µM).

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

体内研究

VU0134992 hydrochloride (50-100 mg/kg; oral gavage) statistically significantly increased urinary Na⁺ as well as K⁺ excretion.

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

Animal Model:	Male Sprague-Dawley rats (250-300 g)
Dosage:	Oral gavage
Administration:	50 and 100 mg/kg
Result:	Statistically significantly increased urinary Na+ as well as K⁺ excretion.

体内研究

VU0134992 hydrochloride (50-100 mg/kg; oral gavage) statistically significantly increased urinary Na⁺ as well as K⁺ excretion.

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

Animal Model:	Male Sprague-Dawley rats (250-300 g)
Dosage:	Oral gavage
Administration:	50 and 100 mg/kg
Result:	Statistically significantly increased urinary Na+ as well as K⁺ excretion.

性状

Solid

溶解性数据

In Vitro:

DMSO : 250 mg/mL (558.24 mM; Need ultrasonic)

H₂O : 2.27 mg/mL (5.07 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.2329 mL	11.1647 mL	22.3294 mL
5 mM	0.4466 mL	2.2329 mL	4.4659 mL
10 mM	0.2233 mL	1.1165 mL	2.2329 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 (sealed storage, away from moisture)。-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 (4.64 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.64 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
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (4.64 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.64 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 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (4.64 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.64 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。