1. GPCR/G Protein Neuronal Signaling
  2. Adrenergic Receptor
  3. Aaptamine

Aaptamine, a spongean alkaloid isolated from a sea sponge Aaptos aaptos, is a competitive antagonist of α-adrenoceptor and activates the p21 promoter in a p53-independent manner.

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Aaptamine Chemical Structure

Aaptamine Chemical Structure

CAS No. : 85547-22-4

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Description

Aaptamine, a spongean alkaloid isolated from a sea sponge Aaptos aaptos, is a competitive antagonist of α-adrenoceptor and activates the p21 promoter in a p53-independent manner[1][1].

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]
Molecular Weight

228.25

Formula

C13H12N2O2

CAS No.
Appearance

Solid

Color

White to yellow

SMILES

COC1=C2C3=C(N=CC=C3C=C1OC)C=CN2

Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

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

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (438.12 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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g

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(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.71%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 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
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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.

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Product Name:
Aaptamine
Cat. No.:
HY-N4225
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