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Nicergoline

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纯度: 99.80%

货号 T1132Cas号 27848-84-6

别名 尼麦角林, Nimergoline, Nicergolinum

Nicergoline (Nicergolinum) 是一种有效的,选择性的、具有口服活性的α1A-肾上腺素能受体拮抗剂,是一种溴烟碱酸的麦角林衍生物。它具有血管舒张作用,可以改善阿尔茨海默症小鼠的认知功能。

Nicergoline
其他形式的 “Nicergoline”:

Nicergoline

一键复制产品信息
Rating icon 很棒

纯度: 99.80%

货号 T1132 别名 尼麦角林, Nimergoline, NicergolinumCas号 27848-84-6

Nicergoline (Nicergolinum) 是一种有效的,选择性的、具有口服活性的α1A-肾上腺素能受体拮抗剂,是一种溴烟碱酸的麦角林衍生物。它具有血管舒张作用,可以改善阿尔茨海默症小鼠的认知功能。

规格价格库存数量
5 mg
¥ 255
现货
10 mg
¥ 413
现货
25 mg
¥ 515
现货
50 mg
¥ 663
现货
100 mg
¥ 1,010
现货
200 mg
¥ 1,530
现货
500 mg
¥ 2,660
现货
1 mL x 10 mM (in DMSO)
¥ 315
现货
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产品介绍


Nicergoline AI Summary
Nicergoline exhibits a diverse range of bioactivities across multiple biological pathways and interactions. This includes notable inhibition of Menin-MLL interaction in MLL-related leukemias, Human Jumonji Domain Containing 2E (JMJD2E), Tyrosyl-DNA Phosphodiesterase (TDP1), Tau fibril formation, and the interaction between CBF-beta and RUNX1 for Acute Myeloid Leukemia treatment. Additionally, it demonstrates effects on lipid storage modulation and vitamin D receptor (VDR) inhibition, along with blocking malaria parasite plastid. The compound also shows potential in blocking the entry of the Ebola virus. In CHO cells transfected with OATP1B3 and OATP1B1, Nicergoline inhibits sodium fluorescein uptake significantly, with inhibition percentages of 124.07% and 91.22% at 10 µM, respectively. However, in assays related to SARS-CoV-2, the results are mixed. It shows limited inhibition of cell viability in Vero E6 cells (inhibition index of -0.08213), some antiviral activity in Caco-2 cells with -11.94% inhibition, and a modest hit score of 0.1321 in HRCE cells. It also exhibits 20.38% inhibition of SARS-CoV-2 3CL-Pro protease activity at 20 µM and no inhibition of cytotoxicity in VERO-6 cells. Furthermore, Nicergoline inhibits human HDAC6 activity but with varying results dependent upon the peptide substrate used: -49.11% inhibition with a commercial substrate versus -0.19% with a custom one. It also exhibits selective binding to receptors like DRD1, KCNH2, and SLC6A3, and shows antagonist activity at TBXA2R while acting as an agonist at ADORA3 and HTR2B. This compound is evaluated for inhibiting enzymes such as ACHE, MAOA, and PTGS1, displaying a broad spectrum of bioactivities affecting numerous receptors and enzymes..
Note: Summary generated by AI. Data source: ChEMBL
生物活性
产品描述
Nicergoline (Nicergolinum) is an ergot derivative used to treat senile dementia and other disorders with vascular origins.
别名尼麦角林, Nimergoline, Nicergolinum
化学信息
分子量484.39
分子式C24H26BrN3O3
CAS No.27848-84-6
SmilesO(C)[C@@]12C=3C=4C(C[C@]1(N(C)C[C@H](COC(=O)C=5C=C(Br)C=NC5)C2)[H])=CN(C)C4C=CC3
密度1.47 g/cm3
颜色White
物理性状Solid
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: 50 mg/mL (103.22 mM), Sonication is recommended.
体内实验配方
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.13 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 mM2.0645 mL10.3223 mL20.6445 mL103.2226 mL
5 mM0.4129 mL2.0645 mL4.1289 mL20.6445 mL
10 mM0.2064 mL1.0322 mL2.0645 mL10.3223 mL
20 mM0.1032 mL0.5161 mL1.0322 mL5.1611 mL
50 mM0.0413 mL0.2064 mL0.4129 mL2.0645 mL
100 mM0.0206 mL0.1032 mL0.2064 mL1.0322 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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