1. Metabolic Enzyme/Protease Neuronal Signaling GPCR/G Protein Anti-infection
  2. Adiponectin Receptor Adrenergic Receptor Reverse Transcriptase
  3. Gramine

Gramine (Donaxine) is a natural alkaloid isolated from giant reed, acts as an active adiponectin receptor (AdipoR) agonist, with IC50s of 3.2 and 4.2 μM for AdipoR2 and AdipoR1, respectively. Gramine is also a human and mouse β2-Adrenergic receptor (β2-AR) agonist. Gramine (Donaxine) has anti-tumor, anti-viral and anti-inflammatory properties.

For research use only. We do not sell to patients.

Gramine Chemical Structure

Gramine Chemical Structure

CAS No. : 87-52-5

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10 mM * 1 mL in DMSO
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Based on 3 publication(s) in Google Scholar

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  • Biological Activity

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Description

Gramine (Donaxine) is a natural alkaloid isolated from giant reed[2], acts as an active adiponectin receptor (AdipoR) agonist, with IC50s of 3.2 and 4.2 μM for AdipoR2 and AdipoR1, respectively[1]. Gramine is also a human and mouse β2-Adrenergic receptor (β2-AR) agonist[2]. Gramine (Donaxine) has anti-tumor, anti-viral and anti-inflammatory properties[1].

IC50 & Target

IC50: 3.2 µM (AdipoR2), 4.2 µM (AdipoR1)[1]

Cellular Effect
Cell Line Type Value Description References
BGC-823 IC50
62.8 μg/mL
Compound: Gramine
Cytotoxicity against human BGC823 cells after 72 hrs by MTT assay
Cytotoxicity against human BGC823 cells after 72 hrs by MTT assay
[PMID: 22647218]
HepG2 IC50
> 100 μg/mL
Compound: Gramine
Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay
Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay
[PMID: 22647218]
NCI-H460 IC50
74.5 μg/mL
Compound: Gramine
Cytotoxicity against human NCI-H460 cells after 72 hrs by MTT assay
Cytotoxicity against human NCI-H460 cells after 72 hrs by MTT assay
[PMID: 22647218]
SGC-7901 IC50
77.3 μg/mL
Compound: Gramine
Cytotoxicity against human SGC7901 cells after 72 hrs by MTT assay
Cytotoxicity against human SGC7901 cells after 72 hrs by MTT assay
[PMID: 22647218]
In Vitro

Gramine is an active adiponectin receptor (AdipoR) agonist, with IC50s of 3.2 and 4.2 μM for AdipoR2 and AdipoR1, respectively[1]. Gramine is a potential β2-AR agonist[2].
Gramine (20 μM to 1.2 nM) dose-dependently inhibits the growth of AdipoR1/adipoR2-positive cancer cell lines (MDA-MB-231 and MCF-7 cells), with IC50s of 9.6±0.9 and 0.1±0.1 μM, respectively[1].

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

Molecular Weight

174.24

Formula

C11H14N2

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CN(C)CC1=CNC2=C1C=CC=C2

Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 125 mg/mL (717.40 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 5.7392 mL 28.6961 mL 57.3921 mL
5 mM 1.1478 mL 5.7392 mL 11.4784 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (11.94 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (11.94 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.63%

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 5.7392 mL 28.6961 mL 57.3921 mL 143.4803 mL
5 mM 1.1478 mL 5.7392 mL 11.4784 mL 28.6961 mL
10 mM 0.5739 mL 2.8696 mL 5.7392 mL 14.3480 mL
15 mM 0.3826 mL 1.9131 mL 3.8261 mL 9.5654 mL
20 mM 0.2870 mL 1.4348 mL 2.8696 mL 7.1740 mL
25 mM 0.2296 mL 1.1478 mL 2.2957 mL 5.7392 mL
30 mM 0.1913 mL 0.9565 mL 1.9131 mL 4.7827 mL
40 mM 0.1435 mL 0.7174 mL 1.4348 mL 3.5870 mL
50 mM 0.1148 mL 0.5739 mL 1.1478 mL 2.8696 mL
60 mM 0.0957 mL 0.4783 mL 0.9565 mL 2.3913 mL
80 mM 0.0717 mL 0.3587 mL 0.7174 mL 1.7935 mL
100 mM 0.0574 mL 0.2870 mL 0.5739 mL 1.4348 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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Gramine
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