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Melperone

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纯度: 98.84%

货号 T7421Cas号 3575-80-2

别名 美哌隆

Melperone 是一种丁酰苯,是一种具有睡眠诱导作用的抗精神病试剂,常用于研究精神类疾病。

Melperone
其他形式的 “Melperone”:

Melperone

一键复制产品信息
Rating icon 很棒

纯度: 98.84%

货号 T7421 别名 美哌隆Cas号 3575-80-2

Melperone 是一种丁酰苯,是一种具有睡眠诱导作用的抗精神病试剂,常用于研究精神类疾病。

规格价格库存数量
2 mg
¥ 108
现货
5 mg
¥ 153
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10 mg
¥ 248
现货
25 mg
¥ 395
现货
50 mg
¥ 548
现货
100 mg
¥ 833
现货
200 mg
¥ 1,230
现货
1 mL x 10 mM (in DMSO)
¥ 172
现货
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纯度: 98.84%
颜色: 黄色
性状: Solid
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产品介绍


Melperone AI Summary
Melperone exhibits a wide range of bioactivities with varying potencies across different assays. It shows significant potency in inhibiting the Menin-MLL interaction in MLL-related leukemias (44668.4 nM) and acts as a delayed death inhibitor of the malarial parasite plastid after a 96-hour incubation (95.3 nM). It demonstrates potencies in promoting Schwann cell viability (40533.4 nM), involvement in a Schwann cell luciferase assay (16136.6 nM), and blocking the entry of Ebola virus with AC50 values of 6309.6 nM and 6.31 µM in different assays. Pharmacokinetically, Melperone shows moderate clearance (46.0 mL·min⁻¹·kg⁻¹), a short half-life (3.9 hours), a moderate mean residence time (5.0 hours), and a moderate volume of distribution at steady state (14.0 L·kg⁻¹) in humans after intravenous administration. The compound exhibits moderate hepatotoxicity, characterized by cytolytic, choleostatic, and mixed liver toxicity, though severe hepatitis and chronic liver conditions have not been linked to it. In antiviral activity assays, Melperone showed mixed results against SARS-CoV-2. It inhibited cytotoxicity in Caco-2 cells by -27.17% at a 10 µM concentration over 48 hours and displayed 16.3% inhibition of the SARS-CoV-2 3CL-Pro protease at 20 µM. However, its IC50 value against SARS-CoV-2 induced cytotoxicity in VERO-6 cells was greater than 20000.0 nM, indicating a relatively weak inhibitory effect. It also demonstrated no significant inhibition of various human transporters (BSEP, MRP2, MRP3, and MRP4) with IC50 values exceeding 133000.0 nM. Additionally, the compound shows minor inhibition rates for human HDAC6, with 18.11% inhibition in one enzymatic assay and -9.44% in another using different peptide substrates. It has bioactivity involving a primary screen assay using NF54 nanoGlo with a Z score of 0.66 and -6.0% inhibition at 2µM over 72 hours. Melperone also interacts with several receptors, including DRD1, DRD3, ADRA2A, HTR1A, and others, with AC50 values from 305.0 nM to 12567.5 nM, showing agonistic activity at HTR2B and ADRA1A receptors (AC50 > 30000.0 nM), and antagonist activity at the TBXA2R receptor (AC50 > 30000.0 nM). These interactions suggest potential effects on neurotransmitter systems and hormone receptors..
Note: Summary generated by AI. Data source: ChEMBL
生物活性
产品描述
Melperone, a butyrophenone tranquillizer, caused bradycardia in vivo and in vitro.
别名美哌隆
化学信息
分子量263.35
分子式C16H22FNO
CAS No.3575-80-2
SmilesCC1CCN(CCCC(=O)c2ccc(F)cc2)CC1
密度1.046 g/cm3 (Predicted)
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: 41.67 mg/mL (158.23 mM), Sonication is recommended.
体内实验配方
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (7.59 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 mM3.7972 mL18.9861 mL37.9723 mL189.8614 mL
5 mM0.7594 mL3.7972 mL7.5945 mL37.9723 mL
10 mM0.3797 mL1.8986 mL3.7972 mL18.9861 mL
20 mM0.1899 mL0.9493 mL1.8986 mL9.4931 mL
50 mM0.0759 mL0.3797 mL0.7594 mL3.7972 mL
100 mM0.0380 mL0.1899 mL0.3797 mL1.8986 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:
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

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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