Home>>Signaling Pathways>> GPCR/G protein>> Adrenergic Receptor>>Aaptamine

Aaptamine Sale

目录号 : GC41327

Aaptamine 是一种从海绵 Aaptos aaptos 中分离出来的海绵类生物碱,是 α-肾上腺素受体的竞争性拮抗剂,以不依赖 p53 的方式激活 p21 启动子。

Aaptamine Chemical Structure

Cas No.:85547-22-4

规格 价格 库存 购买数量
500μg
¥2,131.00
现货
1mg
¥3,117.00
现货

电话:400-920-5774 Email: sales@glpbio.cn

Customer Reviews

Based on customer reviews.

Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

View current batch:

产品描述

Aaptamine is a marine sponge alkaloid originally isolated from A. aaptos with diverse biological activities, including antiproliferative and antidepressant properties. It is an agonist of δ- and μ-opioid receptors (EC50s = 5.1 and 10.1 μM, respectively, in HEK293 cells expressing human recombinant receptors) and a competitive antagonist of α-adrenergic receptors (α-ARs; pA2s = 4.88 and 5.43, respectively, in isolated rabbit aorta and renal artery). Aaptamine inhibits growth of HeLa cervical cancer (IC50 = 15 μg/ml) and K562 leukemia (GI50 = 10 μM) cells and induces cell cycle arrest in the G2/M phase in K562 leukemia and MG63 osteosarcoma cells. It is a proteasome inhibitor that inhibits chymotrypsin-, caspase-, and trypsin-like activity in a partially purified rat liver proteasome preparation (IC50s = 1.6, 2.7, and 18 μg/ml, respectively) and dose-dependently activates p21 independent of p53 in MG63 cells when used at concentrations ranging from 20 to 50 μM. Aaptamine (40 mg/kg, i.p.) decreases immobility time in the forced swim test in mice, indicating antidepressant-like activity.

Chemical Properties

Cas No. 85547-22-4 SDF
Canonical SMILES COC1=C(OC)C=C2C3=C1NC=CC3=NC=C2
分子式 C13H12N2O2 分子量 228.3
溶解度 DMSO: soluble,Ethanol: soluble 储存条件 4°C, protect from light
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。
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。

溶解性数据

制备储备液
1 mg 5 mg 10 mg
1 mM 4.3802 mL 21.901 mL 43.802 mL
5 mM 0.876 mL 4.3802 mL 8.7604 mL
10 mM 0.438 mL 2.1901 mL 4.3802 mL
  • 摩尔浓度计算器

  • 稀释计算器

  • 分子量计算器

质量
=
浓度
x
体积
x
分子量
 
 
 
*在配置溶液时,请务必参考产品标签上、MSDS / COA(可在Glpbio的产品页面获得)批次特异的分子量使用本工具。

计算

动物体内配方计算器 (澄清溶液)

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
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

Research Update

Review on marine sponge alkaloid, Aaptamine: A potential antibacterial and anticancer drug

Chem Biol Drug Des 2022 Jan;99(1):103-110.PMID:34331335DOI:10.1111/cbdd.13932.

In recent years, biological macromolecules have piqued the interest of researchers owing to their vast variety of biological uses. As a result, the marine sponge is a multicellular heterotrophic parazoan with chemicals for defence against predator assaults, biofouling and microbial diseases. These priceless molecules are known as secondary metabolites, and they are essential for survival in a highly competitive environment. So far, over 5,000 marine natural compounds have been extracted from marine sponges, making them an excellent option for drug formulation. One among them is, Aaptamine, a marine alkaloid with a benzo[de][1,6]-napthyridine framework extensively distributed in marine sponges. Due to this reason, Aaptamine has been intensively researched for various biological purposes, including cancer and protease inhibition, offering fresh insights into novel treatments. Keeping this in mind, we reviewed the biological significance of the marine sponge alkaloid Aaptamine.

Aaptamine - a dual acetyl - and butyrylcholinesterase inhibitor as potential anti-Alzheimer's disease agent

Pharm Biol 2022 Dec;60(1):1502-1510.PMID:35968601DOI:10.1080/13880209.2022.2102657.

Context: Alzheimer's disease (AD) is a neurodegenerative disorder that affects millions of people worldwide. Acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) are promising therapeutic targets for AD. Objective: To evaluate the inhibitory effects of Aaptamine on two cholinesterases and investigate the in vivo therapeutic effect on AD in a zebrafish model. Materials and methods: Aaptamine was isolated from the sponge Aaptos suberitoides Brøndsted (Suberitidae). Enzyme inhibition, kinetic analysis, surface plasmon resonance (SPR) and molecular docking assays were used to determine its inhibitory effect on AChE and BuChE in vitro. Zebrafish were divided into six groups: control, model, 8 μM donepezil, 5 , 10 and 20 μM Aaptamine. After three days of drug treatment, the behaviour assay was performed. Results: The IC50 values of Aaptamine towards AChE and BuChE were 16.0 and 4.6 μM. And Aaptamine directly inhibited the two cholinesterases in the mixed inhibition type, with Ki values of 6.96 ± 0.04 and 6.35 ± 0.02 μM, with Kd values of 87.6 and 10.7 μM. Besides, Aaptamine interacts with the crucial anionic sites of AChE and BuChE. In vivo studies indicated that the dyskinesia recovery rates of 5 , 10 and 20 μM Aaptamine group were 34.8, 58.8 and 60.0%, respectively, and that of donepezil was 63.7%. Discussion and conclusions: Aaptamine showed great potential to exert its anti-AD effects by directly inhibiting the activities of AChE and BuChE. Therefore, this study identified a novel medicinal application of Aaptamine and provided a new structural scaffold for the development of anti-AD drugs.

Four new Aaptamine alkaloids from marine sponge Aaptos aaptos

Nat Prod Res 2022 Oct;36(19):5022-5031.PMID:33908314DOI:10.1080/14786419.2021.1917572.

Four new Aaptamine alkaloids, named as 9-methoxy-N-demethylaaptanone (1), 3,5-dicarbomethoxy-1,​6-​naphthyridine (2), aaptosvanphongs A and B (3 and 4), and three known Aaptamine alkaloids as 2-methoxy-3-oxoaaptamine (5), 8,9,9-trimethoxy-9H-benzo[de][1,6]-naphthyridine (6), and demethyl(oxy)Aaptamine (7) were isolated from the sponge Aaptos by various chromatographic methods. Their structures were established by extensive spectroscopic analyses (HR-ESI-MS, 1 D and 2 D NMR) and by comparison of the spectral data with those reported in the literature. Compounds 1-7 significantly showed cytotoxic effects against SK-LU-1, MCF-7, HepG2, and SK-Mel-2 cell lines with IC50 values in range from 7.7 ± 0.8 to 51.4 ± 1.8 µM. Among them, compound 7 exhibited the most cytotoxic activity with corresponding IC50 values of 9.2 ± 1.0, 7.8 ± 0.6, 8.4 ± 0.8, and 7.7 ± 0.8 µM.[Formula: see text].

Aaptamine attenuates the proliferation and progression of non-small cell lung carcinoma

Pharm Biol 2020 Dec;58(1):1044-1054.PMID:33027592DOI:10.1080/13880209.2020.1822420.

Context: Aaptamine is a potent ocean-derived non-traditional drug candidate against human cancers. However, the underlying molecular mechanisms governing aaptamine-mediated repression of lung cancer cells remain largely undefined. Objective: To examine the inhibitory effect of Aaptamine on proliferation and progression of non-small cell lung carcinoma (NSCLC) and dissect the potential mechanisms involved in its anticancer functions. Materials and methods: In vitro assays of cell proliferation, cell cycle analysis, clonal formation, apoptosis and migration were performed to examine the inhibitory effects of Aaptamine (8, 16 and 32 μg/mL) on NSCLC cells. The expression levels of proteins were analysed using western blotting analysis when cells were treated with a single drug or a combination treatment for 48 h. Results: Aaptamine significantly inhibited A549 and H1299 cells proliferation with IC50 values of 13.91 and 10.47 μg/mL. At the concentrations of 16 and 32 μg/mL, Aaptamine significantly reduced capacities in clonogenicity, enhanced cellular apoptosis and decreased the motile and invasive cellular phenotype. In addition, Aaptamine arrested cell cycle at G1 phase via selectively abating cell cycle regulation drivers (CDK2/4 and Cyclin D1/E). Western blotting results showed that Aaptamine attenuated the protein expression of MMP-7, MMP-9 and upregulated the expression of cleaved-PARP and cleaved-caspase 3. Moreover, Aaptamine inhibited PI3K/AKT/GSK3β signalling cascades through specifically degrading the phosphorylated AKT and GSK3β. Discussion and conclusions: Aaptamine retarded the proliferation and invasion of NSCLC cells by selectively targeting the pathway PI3K/AKT/GSK3β suggesting it as a potential chemotherapeutic agent for repressing tumorigenesis and progression of NSCLC in humans.

Antinociceptive Effects of Aaptamine, a Sponge Component, on Peripheral Neuropathy in Rats

Mar Drugs 2023 Feb 4;21(2):113.PMID:36827154DOI:10.3390/md21020113.

Aaptamine, a natural marine compound isolated from the sea sponge, has various biological activities, including delta-opioid agonist properties. However, the effects of Aaptamine in neuropathic pain remain unclear. In the present study, we used a chronic constriction injury (CCI)-induced peripheral neuropathic rat model to explore the analgesic effects of intrathecal Aaptamine administration. We also investigated cellular angiogenesis and lactate dehydrogenase A (LDHA) expression in the ipsilateral lumbar spinal cord after Aaptamine administration in CCI rats by immunohistofluorescence. The results showed that Aaptamine alleviates CCI-induced nociceptive sensitization, allodynia, and hyperalgesia. Moreover, Aaptamine significantly downregulated CCI-induced vascular endothelial growth factor (VEGF), cluster of differentiation 31 (CD31), and LDHA expression in the spinal cord. Double immunofluorescent staining showed that the spinal VEGF and LDHA majorly expressed on astrocytes and neurons, respectively, in CCI rats and inhibited by Aaptamine. Collectively, our results indicate Aaptamine's potential as an analgesic agent for neuropathic pain. Furthermore, inhibition of astrocyte-derived angiogenesis and neuronal LDHA expression might be beneficial in neuropathy.