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Pinacidil

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纯度: 99.9%

货号 T12478LCas号 60560-33-0

别名 吡那地尔, S-1230, S 1230, P-1134, P1134, P 1134

Pinacidil (P 1134) 是钾通道的有效激活剂。Pinacidil 通过打开 K+-通道使血管平滑肌超极化,显示出抗高血压活性。它显著改善再灌注功能和心脏顺应性。它具有直接的心脏保护作用。

Pinacidil
其他形式的 “Pinacidil”:

Pinacidil

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Rating icon 很棒

纯度: 99.9%

货号 T12478L 别名 吡那地尔, S-1230, S 1230, P-1134, P1134, P 1134Cas号 60560-33-0

Pinacidil (P 1134) 是钾通道的有效激活剂。Pinacidil 通过打开 K+-通道使血管平滑肌超极化,显示出抗高血压活性。它显著改善再灌注功能和心脏顺应性。它具有直接的心脏保护作用。

规格价格库存数量
1 mg
¥ 197
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5 mg
¥ 417
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10 mg
¥ 587
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25 mg
¥ 997
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50 mg
¥ 1,685
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100 mg
¥ 2,530
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1 mL x 10 mM (in DMSO)
¥ 460
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产品介绍


Pinacidil AI Summary
Pinacidil exhibits a range of bioactivities relating to muscle relaxation, insulin secretion, and cardiovascular effects. It has potent vasorelaxant properties, with an EC50 of 724.44 nM and high intrinsic activity of 91.9% in relaxing rat aorta precontracted with KCl. Additionally, it inhibits the contraction of rat detrusor strips with an IC50 of 630.0 nM and demonstrates significant relaxant activities in various smooth muscles, including the rat aorta and guinea pig trachea. In terms of insulin secretion, Pinacidil inhibits glucose-stimulated insulin release from rat islets, with an IC50 value greater than 100,000 nM. It also demonstrates inhibitory activity in specific cellular assays, such as inhibiting ATP-dependent taurocholate uptake in human BSEP with an IC50 of 348,100 nM. Pinacidil shows antihypertensive effects in animal models, including significant reductions in blood pressure in spontaneously hypertensive rats and hypertensive dogs. It demonstrates efficacy in various vasorelaxant and potassium channel activities, suggesting potential therapeutic benefits in cardiovascular treatments. Additionally, the compound exhibits selective bioactivities related to its interaction with potassium channels, showing a significant effect on ATP-sensitive potassium channels (KATP) in different smooth muscle and pancreatic islet cells. Overall, Pinacidil presents a promising profile as a vasorelaxant and antihypertensive agent, while also affecting glucose-induced insulin secretion and demonstrating significant interaction with potassium channels..
Note: Summary generated by AI. Data source: ChEMBL
生物活性
产品描述
Pinacidil (P 1134) is a guanidine that opens potassium channels and directly dilates peripheral blood vessels in small arteries, lowering blood pressure and peripheral resistance and producing fluid retention.
别名吡那地尔, S-1230, S 1230, P-1134, P1134, P 1134
化学信息
分子量245.32
分子式C13H19N5
CAS No.60560-33-0
SmilesCC(N\C(Nc1ccncc1)=N/C#N)C(C)(C)C
密度1.1402 g/cm3 (Estimated)
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
溶解度信息
DMSO: 100 mg/mL (407.63 mM), Sonication is recommended.
体内实验配方
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (16.31 mM), Sonication is recommended.
请按顺序添加溶剂,在添加下一种溶剂之前,尽可能使溶液澄清。如有必要,可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考,体内配方并不是绝对的,请根据不同情况进行调整。
溶液配制表
DMSO
1mg5mg10mg50mg
1 mM4.0763 mL20.3815 mL40.7631 mL203.8154 mL
5 mM0.8153 mL4.0763 mL8.1526 mL40.7631 mL
10 mM0.4076 mL2.0382 mL4.0763 mL20.3815 mL
20 mM0.2038 mL1.0191 mL2.0382 mL10.1908 mL
50 mM0.0815 mL0.4076 mL0.8153 mL4.0763 mL
100 mM0.0408 mL0.2038 mL0.4076 mL2.0382 mL

计算器

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体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法:
比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL, 一共给药动物10只,您使用的配方为 10% DMSO + 40% PEG300 + 5% Tween 80 + 45% Saline / PBS / ddH2O, 那么您的工作液浓度为2 mg/mL
母液配置方法:2 mg 药物溶于 100 μL DMSO ( 母液浓度为 20 mg/mL ), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:100 μL DMSO 母液, 添加 400 μL PEG300 混匀澄清, 再加 50 μL Tween 80, 混匀澄清, 再加 450 μL Saline / PBS / ddH2O 混匀澄清
以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。
方案所需的各类助溶剂如: DMSOPEG300PEG400Tween 80SBE-β-CD玉米油等, 均可在TargetMol网站点击购买。
1 请输入动物实验的基本信息
mg/kg
g
μL
2 请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

剂量转换

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