2. GPCR/G Protein Neuronal Signaling Metabolic Enzyme/Protease Anti-infection Apoptosis Immunology/Inflammation NF-κB
  3. Adrenergic Receptor Proteasome Cholinesterase (ChE) Bacterial Apoptosis AP-1 NF-κB
  4. Aaptamine

Aaptamine 是一种可从海绵 Aaptos suberitoides 中分离得到的生物碱。Aaptamine 是 α-肾上腺素受体竞争性拮抗剂、蛋白酶体和胆碱酯酶抑制剂。Aaptamine 对肿瘤细胞具有细胞毒性，可诱导肿瘤细胞凋亡 (apoptosis) 、细胞周期阻滞，以及通过 p53 非依赖途径诱导 p21 表达。Aaptamine 具有抗肿瘤、抗氧化、抗菌和镇痛等多种活性。

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Aaptamine Chemical Structure

Aaptamine Chemical Structure

CAS No. : 85547-22-4

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规格 价格 是否有货
1 mg ￥3050
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Customer Review

Aaptamine 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 1 篇科研文献

查看 Adrenergic Receptor 亚型特异性产品:

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α adrenergic receptor β adrenergic receptor

查看 Cholinesterase (ChE) 亚型特异性产品:

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AChE BChE

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c-Fos c-Jun

查看 NF-κB 亚型特异性产品:

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Aaptamine is an alkaloid that can be isolated from the sponge Aaptos suberitoides. Aaptamine is a competitive antagonist of the α-adrenergic receptor, as well as an inhibitor of the proteasome and cholinesterase. Aaptamine is cytotoxic to tumor cells and can induce apoptosis, cell cycle arrest of tumor cells, and the expression of p21 through a p53-independent pathway. Aaptamine has multiple activities such as anti-tumor, antioxidant, antibacterial, and analgesic effects[1][2][3][4][5][6][7].

IC50 & Target[5]

AChE

0.23 μg/mL (IC50)

BChE

1.38 μg/mL (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
786-0 EC50
> 100 μM
Compound: 1
Inhibition of HIF2alpha in human 786-0 cells expressing truncated HIF1alpha assessed as reduction in luciferase activity after 24 hrs by reporter gene assay
Inhibition of HIF2alpha in human 786-0 cells expressing truncated HIF1alpha assessed as reduction in luciferase activity after 24 hrs by reporter gene assay
[PMID: 22928967]
A549 IC50
2.8 μg/mL
Compound: 2
Cytotoxicity against human A549 cells after 6 days by MTT assay
Cytotoxicity against human A549 cells after 6 days by MTT assay
[PMID: 10514310]
HeLa IC50
15 μg/mL
Compound: 1
Cytotoxicity against human HeLa cells after 3 days by MTT assay
Cytotoxicity against human HeLa cells after 3 days by MTT assay
[PMID: 20451377]
HeLa IC50
19 μM
Compound: 1
Cytotoxicity against human HeLa cells assessed as reduction in cell viability after 48 hrs by CCK8 assay
Cytotoxicity against human HeLa cells assessed as reduction in cell viability after 48 hrs by CCK8 assay
[PMID: 33170001]
HL-60 IC50
> 55 μM
Compound: 7
Antioxidant activity against TPA-induced ROS production in human HL60 cells by 2',7'-dichlorodihydrofluorescein diacetate cellular-based assay
Antioxidant activity against TPA-induced ROS production in human HL60 cells by 2',7'-dichlorodihydrofluorescein diacetate cellular-based assay
[PMID: 12762791]
HT-29 IC50
6.9 μg/mL
Compound: 2
Cytotoxicity against human HT-29 cells after 6 days by MTT assay
Cytotoxicity against human HT-29 cells after 6 days by MTT assay
[PMID: 10514310]
L5178Y IC50
8.3 μM
Compound: 5
Cytotoxic activity against mouse L5178Y cells by MTT assay
Cytotoxic activity against mouse L5178Y cells by MTT assay
[PMID: 23282083]
MCF7 IC50
> 20 μM
Compound: 1
Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by CCK8 assay
Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by CCK8 assay
[PMID: 33170001]
NB-4 IC50
> 20 μM
Compound: 1
Cytotoxicity against human NB4 cells assessed as reduction in cell viability after 48 hrs by CCK8 assay
Cytotoxicity against human NB4 cells assessed as reduction in cell viability after 48 hrs by CCK8 assay
[PMID: 33170001]
P388 IC50
0.6 μg/mL
Compound: 2
Cytotoxicity against mouse P388 cells after 3 days by MTT assay
Cytotoxicity against mouse P388 cells after 3 days by MTT assay
[PMID: 10514310]
体外研究
(In Vitro)

Aaptamine (10 μM) 在兔离体主动脉和肾动脉中可使去甲肾上腺素的剂量-反应曲线平行右移，而对组胺或氯化钾曲线无影响[1]。
Aaptamine (30 μg/mL; 0-48 h) 在 MG63 细胞中可增加 p21 的表达，并诱导细胞周期阻滞[2]。
Aaptamine (3 days) 对 HeLa 细胞具有细胞毒性，IC50 为 15 μg/mL[3]。
Aaptamine (50-100 μM; 6-24 h) 在 JB6 Cl41 细胞中可激活 AP-1 和 NF-κB 依赖的转录活性[4]。
Aaptamine (5-55 µg/mL; 24 h) 对产 ESBL 的革兰氏阴性尿路致病菌具有抑制作用[6]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Aaptamine 相关抗体:

Western Blot Analysis[2]

Cell Line: MG63 cells
Concentration: 30 μg/mL
Incubation Time: 0, 3, 6, 12, 24 and 48 h
Result: Increased the level of p21.
体内研究
(In Vivo)

Aaptamine (5-100 μg; 鞘内注射; 单次) 在慢性压迫损伤 (CCI) 诱导的周围神经病变大鼠模型中具有镇痛的作用[7]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Chronic constriction injury treated adult male Wistar rats (250-285 g)[7]
Dosage: 5, 30 and 100 μg
Administration: Intrathecal injection; single dose
Result: Showed different durations of analgesic effects on CCI-induced nociception. The 5 μg, 30 μg, and 100 μg doses presented analgesic durations of 90, 150, and 150 minutes respectively. However, the variance in the group administered with 100 μg of aaptamine was the largest, and the rats presented some abnormal motor behavior.
分子量

228.25

Formula

C13H12N2O2
CAS 号
性状

固体

颜色

White to yellow

结构分类
初始来源

sponge
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
细胞实验： 

DMSO 中的溶解度 : 100 mg/mL (438.12 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 4.3812 mL 21.9058 mL 43.8116 mL
5 mM 0.8762 mL 4.3812 mL 8.7623 mL
查看完整储备液配制表

* 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, 6 months; -20°C, 1 month (protect from light)。-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。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 99.71%

COA (292 KB) HNMR (203 KB) LCMS (92 KB)

产品使用指南 (1538 KB)
参考文献

Aaptamine 相关分类

完整储备液配制表

* 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, 6 months; -20°C, 1 month (protect from light)。-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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 4.3812 mL 21.9058 mL 43.8116 mL 109.5290 mL
5 mM 0.8762 mL 4.3812 mL 8.7623 mL 21.9058 mL
10 mM 0.4381 mL 2.1906 mL 4.3812 mL 10.9529 mL
15 mM 0.2921 mL 1.4604 mL 2.9208 mL 7.3019 mL
20 mM 0.2191 mL 1.0953 mL 2.1906 mL 5.4765 mL
25 mM 0.1752 mL 0.8762 mL 1.7525 mL 4.3812 mL
30 mM 0.1460 mL 0.7302 mL 1.4604 mL 3.6510 mL
40 mM 0.1095 mL 0.5476 mL 1.0953 mL 2.7382 mL
50 mM 0.0876 mL 0.4381 mL 0.8762 mL 2.1906 mL
60 mM 0.0730 mL 0.3651 mL 0.7302 mL 1.8255 mL
80 mM 0.0548 mL 0.2738 mL 0.5476 mL 1.3691 mL
100 mM 0.0438 mL 0.2191 mL 0.4381 mL 1.0953 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Aaptamine85547-22-4Adrenergic ReceptorProteasomeCholinesterase (ChE)BacterialApoptosisAP-1NF-κBBeta ReceptorActivator Protein 1Nuclear factor-κBNuclear factor-kappaBperipheral neuropathy modelMG63 cellsHeLa cellsJB6 Cl41 cellsGram-negative uropathogenic bacteriaInhibitorinhibitorinhibit

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