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Pirenperone

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纯度: 99.2%

货号 T2599Cas号 75444-65-4

别名 匹仑哌隆

Pirenperone 是5-HT2血清素受体拮抗剂,具有一定抗焦虑作用。

Pirenperone
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Pirenperone

一键复制产品信息
Rating icon 很棒

纯度: 99.2%

货号 T2599 别名 匹仑哌隆Cas号 75444-65-4

Pirenperone 是5-HT2血清素受体拮抗剂,具有一定抗焦虑作用。

规格价格库存数量
1 mg
¥ 369
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5 mg
¥ 986
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10 mg
¥ 1,550
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25 mg
¥ 2,970
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50 mg
¥ 4,320
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100 mg
¥ 6,120
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产品介绍


Pirenperone AI Summary
Pirenperone exhibits bioactivity primarily related to serotonin receptors, demonstrating high binding affinity to the 5-HT2 receptor subtype in rat cortical membranes, with Ki values as low as 0.3 nM and moderate affinity for the 5-HT2C receptor subtype with a Ki value of 60 nM. It also shows lower binding affinity to 5-HT1A and 5-HT1B receptor subtypes. Additionally, it acts as a potent inhibitor of membrane-bound and solubilized receptors in rat frontal cortex, with IC50 values of 1.82 nM and 7.079 nM, respectively, pointing to high receptor affinity. However, Pirenperone exhibits notable cardiotoxicity in Dunkin-Hartley guinea pigs, significantly prolonging the QTc interval. Moreover, the compound displays broad-spectrum bioactivity, including antiplasmodial effects against Plasmodium falciparum with IC50 values ranging from 6309.57 nM to 12589.25 nM and activity against other pathogens including Leishmania, Chagas disease, and HAT with varying IC50 values. It also shows antiviral capabilities, inhibiting SARS-CoV-2 induced cytotoxicity in VERO-6 cells and specifically targeting the SARS-CoV-2 3CL-Pro protease enzyme. Moreover, it possesses antifungal and antibacterial activities, albeit with modest inhibition percentages. Despite its diverse bioactivities, Pirenperone has weak inhibitory effects on the human HDAC6 enzyme, with minimal inhibition percentages observed. These extensive biological interactions suggest that Pirenperone may have potential therapeutic applications but also significant safety considerations..
Note: Summary generated by AI. Data source: ChEMBL
生物活性
产品描述
Pirenperone is a putative 5-HT2 receptor antagonist with the central antiserotonergic and antidopaminergic action.
别名匹仑哌隆
化学信息
分子量393.45
分子式C23H24FN3O2
CAS No.75444-65-4
SmilesO=C1N2C(=NC(C)=C1CCN3CCC(C(=O)C4=CC=C(F)C=C4)CC3)C=CC=C2
密度1.26g/cm3
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: 3.67 mg/mL (9.33 mM), Sonication is recommended.
溶液配制表
DMSO
1mg5mg10mg50mg
1 mM2.5416 mL12.7081 mL25.4162 mL127.0810 mL
5 mM0.5083 mL2.5416 mL5.0832 mL25.4162 mL

计算器

  • 摩尔浓度 计算器
  • 稀释 计算器
  • 配液 计算器
  • 分子量 计算器

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:
TargetMol | Animal experiments 比如您的给药剂量是10 mg/kg,每只动物体重20g,给药体积100 μLTargetMol | Animal experiments 一共给药动物10只,您使用的配方为5%TargetMol | reagent DMSO + 30%PEG300 + 5%Tween 80 + 60%Saline/PBS/ddH2O, 那么您的工作液浓度为2mg/mL
母液配置方法: 2 mg 药物溶于 50 μLDMSOTargetMol | reagent ( 母液浓度为 40 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:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween80, 混匀澄清,再加 600μLSaline/PBS/ddH2OTargetMol | reagent 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: DMSOPEG300 / PEG400Tween 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

对于不同动物的给药剂量换算,您也可以参考 更多

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