Ferulamide
(Synonyms: 阿魏酸酰胺) 目录号 : GC60165
Ferulamide是从PortulacaoleraceaL.中分离的具有抗胆碱酯酶活性的阿魏酸衍生物。
Cas No.:61012-31-5
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Ferulamide is a Ferulic acid derivative isolated from Portulaca oleracea L. with anticholinesterase activities[1][2].
[1]. Fen Xiu, et al. A New Alkaloid From Portulaca oleracea L. And Its Antiacetylcholinesterase Activity. Nat Prod Res. 2019 Sep;33(18):2583-2590. [2]. Chun-Jen Chen, et al. (2E)-N,N-dibutyl-3-(4-hydroxy-3-methoxyphenyl)acrylamide Induces Apoptosis and Cell Cycle Arrest in HL-60 Cells. Anticancer Res. Jan-Feb 2007;27(1A):343-9.
| Cas No. | 61012-31-5 | SDF | |
| 别名 | 阿魏酸酰胺 | ||
| Canonical SMILES | O=C(N)/C=C/C1=CC=C(O)C(OC)=C1 | ||
| 分子式 | C10H11NO3 | 分子量 | 193.2 |
| 溶解度 | 储存条件 | ||
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 5.176 mL | 25.8799 mL | 51.7598 mL |
| 5 mM | 1.0352 mL | 5.176 mL | 10.352 mL |
| 10 mM | 0.5176 mL | 2.588 mL | 5.176 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Design, synthesis, and evaluation of novel O-alkyl Ferulamide derivatives as multifunctional ligands for treating Alzheimer's disease
J Enzyme Inhib Med Chem 2022 Dec;37(1):1375-1388.PMID:35549612DOI:10.1080/14756366.2022.2073442.
Herein, a series of novel O-alkyl Ferulamide derivatives were designed and synthesised through the multi-target-directed ligands (MTDLs) strategy. The biological activities in vitro showed that compounds 5a, 5d, 5e, 5f, and 5h indicated significantly selective MAO-B inhibitory potency (IC50 = 0.32, 0.56, 0.54, 0.73, and 0.86 μM, respectively) and moderate antioxidant activity. Moreover, compounds 5a, 5d, 5e, 5f, and 5h showed potent anti-inflammatory properties, remarkable effects on self-induced Aβ1-42 aggregation, and potent neuroprotective effect on Aβ1-42-induced PC12 cell injury. Furthermore, compounds 5a, 5d, 5e, 5f, and 5h presented good blood-brain barrier permeation in vitro and drug-like properties. More interesting, the PET/CT images with [11C]5f demonstrated that [11C]5f could penetrate the BBB with a high brain uptake and exhibited good brain clearance kinetic property. Therefore, compound 5f would be a promising multi-functional agent for the treatment of AD.
Design, synthesis and biological evaluation of novel O-carbamoyl Ferulamide derivatives as multi-target-directed ligands for the treatment of Alzheimer's disease
Eur J Med Chem 2020 May 15;194:112265.PMID:32240904DOI:10.1016/j.ejmech.2020.112265.
A novel series of O-carbamoyl Ferulamide derivatives were designed by multitarget-directed ligands (MTDLs) strategy, the derivatives were synthesized and evaluated to treat Alzheimer's disease (AD). In vitro biological evaluation demonstrated that compound 4f was the best pseudo-irreversible hBChE (human butyrylcholinesterase) inhibitor with an IC50 value of 0.97 μM 4f was a potent selective MAO-B (monoamine oxidase-B) inhibitor (IC50 = 5.3 μM), and could inhibit (58.2%) and disaggregate (43.3%) self-mediated Aβ aggregation. 4f also could reduce the levels of pathological tau and APP clearance, and displayed a wide safe range hepatotoxicity on LO2 cells. The in vivo studies revealed that 4f exhibited fascinating dyskinesia recovery rate and response efficiency on AlCl3-mediated zebrafish, and demonstrated significant protective effect on vascular injury caused by Aβ1-40. PET-CT imaging demonstrated that [11C]4f exhibited high BBB penetration (especially could reach to hippocampus and striatum of brain) and had a fast brain uptake after intravenous bolus injection. Furthermore, compound 4f could improve scopolamine-induced cognitive impairment. Further, the metabolism in vitro of 4f was also investigated, and presented 3 metabolites in rat liver microsome metabolism, 4 metabolites in human liver microsome, and 4 metabolites in rat intestinal flora, providing previous data for the preclinical study. Therefore, these results implied that compound 4f was an advanced multi-function agent and deserved further preclinical study against mild-to-serve Alzheimer's disease.
Identification of (-)(E)-N-[2(S)-Hydroxy-2-(4-hydroxyphenyl) ethyl]Ferulamide, a natural product isolated from Croton pullei: theoretical and experimental analysis
Int J Mol Sci 2011;12(12):9389-403.PMID:22272139DOI:10.3390/ijms12129389.
Ferulic acid (FA) and its derivatives (FADs) are known for a variety of biological activities, such as photo-protective agent, antioxidant, antiatherogenic and antiplasmodial activities. During structural definition of a FAD isolated from Croton pullei, the possibility of a heterologous series made this definition difficult. In this regard, computational simulations were performed using theoretical calculations at DFT level to predict Infrared (IR) and Nuclear Magnetic Resonance (NMR) data. The IR and NMR (13)C and (1)H data were compared with the theoretical calculations performed for three structural possibilities of a heterologous series. The theoretical results were compared with the experimental data through linear regression in order to define the most probable structure and showed satisfactory values.
[Chemical Constituents from Cynanchum paniculatum]
Zhong Yao Cai 2015 Jan;38(1):97-100.PMID:26214877doi
Objective: To investigate the chemical constituents from Gynanchum paniculatum. Methods: The constituents were isolated and purified by silica gel, Sephadex LH-20 column chromatography, and preparative TLC. Their structures were identified on the basis of spectral data and physiochemical characteristics. Results: 15 compounds were isolated from 70% ethanol extract and identified as β-sitosterol(1), β-daucosterin (2), mudanoside A (3), paeonolide (4), santamarin (5), paeonol(6), annobraine (7), laricircsinol (8), α-asarone(9), 7-angelyheliotridine(10), β-amyrin(11), uridine(12), kaempferol-3-O-β-D-glucopyranosyl(1→2)α-L-arabinopyranoside(13), kaempferol-7-O-(4", 6"-di-p-hydroxycinnamoyl-2", 3"-diacetyl)-β-D-glucopyranoside(14), and (2S, E)-N-[2-hydroxy-2-(4-hydroxyphenyl) ethyl] Ferulamide (15). Conclusion: Compounds 4, 6, 8, 11, 12 and 15 are isolated from this plant for the first time, compounds 5 and 14 are firstly isolated from the palnts of Cynanchum genus.
Antioxidative compounds isolated from safflower (Carthamus tinctorius L.) oil cake
Chem Pharm Bull (Tokyo) 1997 Dec;45(12):1910-4.PMID:9433760DOI:10.1248/cpb.45.1910.
Seven antioxidative serotonin derivatives were isolated from safflower (Carthamus tinctorius L.) oil cake. Their structures were established as N-[2-(5-hydroxy-1H-indol-3-yl)ethyl]Ferulamide (1), N-[2-(5-hydroxy-1H-indol-3-yl)ethyl]-p-coumaramide (2), N,N'-[2,2'-(5,5'-dihydroxy-4,4'-bi-1H-indol-3,3'-yl)diethyl]- di-p-coumaramide (3), N-[2-[3'-[2-(p-coumaramido)ethyl]-5,5'-dihydroxy- 4,4'-bi-1H-indol-3-yl]ethyl]Ferulamide (4), and N,N'-[2,2'-(5,5'-dihydroxy-4,4'-bi-1H-indol-3,3'-yl)diethyl]- diferulamide (5), N-[2-[5-(beta-D-glucosyloxy)-1H-indol-3-yl)ethyl]- p-coumaramide (6), and N-[2-[5-(beta-D-glucosyloxy)-1H-indol-3-yl)ethyl]Ferulamide (7). Antioxidative activities of the compounds were measured by the ferric thiocyanate method and the alpha,alpha-diphenyl-beta-picrylhydrazyl (DPPH) method, and compounds 1-5 were found to have relatively strong antioxidative activity.