1. Neuronal Signaling Immunology/Inflammation Metabolic Enzyme/Protease
  2. Imidazoline Receptor NO Synthase Endogenous Metabolite
  3. Agmatine sulfate

Agmatine sulfate exerts modulatory action at multiple molecular targets, such as neurotransmitter systems, ion channels and nitric oxide synthesis. It is an endogenous agonist at imidazoline receptor and a NO synthase inhibitor.

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Agmatine sulfate Chemical Structure

Agmatine sulfate Chemical Structure

CAS No. : 2482-00-0

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in Water
ready for reconstitution
USD 55 In-stock
Solution
10 mM * 1 mL in Water USD 55 In-stock
Solid
100 mg USD 50 In-stock
500 mg USD 70 In-stock
1 g USD 80 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

Agmatine sulfate exerts modulatory action at multiple molecular targets, such as neurotransmitter systems, ion channels and nitric oxide synthesis. It is an endogenous agonist at imidazoline receptor and a NO synthase inhibitor.

IC50 & Target

Human Endogenous Metabolite

 

In Vitro

Agmatine binds to alpha 2-adrenergic and imidazoline receptors and stimulates release of catecholamines from adrenal chromaffin cells. Its biosynthetic enzyme, arginine decarboxylase, is present in brain. Agmatine, locally synthesized, is an endogenous agonist at imidazoline receptors, a noncatecholamine ligand at alpha 2-adrenergic receptors and may act as a neurotransmitter[1]. Agmatine is synthesized in the brain, stored in synaptic vesicles in regionally selective neurons, accumulated by uptake, released by depolarization, and inactivated by agmatinase. Agmatine inhibits nitric oxide synthase, and induces the release of some peptide hormones[2]. Agmatine, 4-(aminobutyl)guanidine, is produced by decarboxylation of L-arginine by the enzyme arginine decarboxylase. Agmatine is a competitive inhibitor of all NOS isoenzymes but not an NO precursor. Ki values are approximately 660 μM (NOS I), 220 μM (NOS II) and 7.5 mM (NOS III)[3]. Agmatine stimulates nitrite production three-fold above basal nitrite formation by endothelial cells. Agmatine displaces [3H]-idazoxan from endothelial cellmembranes and is found to induce transients in the cytosolic calcium of endothelial cells. The transients could be downregulated by repeated exposure to agmatine but are not affected by pretreatment with norepinephrine[4].

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

In Vivo

Agmatine produces an antidepressant-like effect when assessed in the forced swimming test and in the tail suspension test in mice (dose range 0.01-50 mg/kg, i.p.), without accompanying changes in ambulation in an open-field[5]. In ischemic stroke, agmatine protects the blood-brain barrier, which can be monitored in vivo by quantification of permeability by using dynamic contrast-enhanced MR imaging[6]. Agmatine substantially augments the antidepressant-like effect of MK-801, reinforcing the notion that this compound modulates NMDA receptor activation[7].

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

Molecular Weight

228.27

Formula

C5H16N4O4S

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

NC(NCCCCN)=N.O=S(O)(O)=O

Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

H2O : ≥ 100 mg/mL (438.08 mM)

DMSO : < 1 mg/mL (insoluble or slightly soluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.3808 mL 21.9039 mL 43.8078 mL
5 mM 0.8762 mL 4.3808 mL 8.7616 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • 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:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  PBS

    Solubility: 25 mg/mL (109.52 mM); Clear solution; Need ultrasonic and warming

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

Dosage

mg/kg

Animal weight
(per animal)

g

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(per animal)

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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).
Purity & Documentation
References
Animal Administration
[6][7]

Rats: Thirty-four male Sprague-Dawley rats are subjected to transient MCA occlusion for 90 minutes. Immediately after reperfusion, agmatine (100 mg/kg) or normal saline is injected intraperitoneally into the agmatine-treated group (n= 17) or the control group, respectively. MR imaging is performed after reperfusion[6].

Mice: Mice are pretreated with a range of sub-effective doses of either fluoxetine (1, 2.5 and 5 mg/kg, p.o.; a selective serotonin reuptake inhibitor), imipramine (0.01, 0.05 and 0.1 mg/kg, p.o.; a tricyclic antidepressant), bupropion (0.1, 0.5 and 1 mg/kg, p.o.; dopamine reuptake inhibitor with subtle activity on noradrenergic reuptake), or MK-801 (0.0001, 0.0005 and 0.001 mg/kg, p.o.; noncompetitive NMDA receptor antagonist) and immediately after, a sub-effective dose of either agmatine (0.0001 mg/kg p.o.) or vehicle is administered. After 60 min, the animals are subjected to behavioral testing[7].

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

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 (sealed storage, away from moisture). 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
H2O 1 mM 4.3808 mL 21.9039 mL 43.8078 mL 109.5194 mL
5 mM 0.8762 mL 4.3808 mL 8.7616 mL 21.9039 mL
10 mM 0.4381 mL 2.1904 mL 4.3808 mL 10.9519 mL
15 mM 0.2921 mL 1.4603 mL 2.9205 mL 7.3013 mL
20 mM 0.2190 mL 1.0952 mL 2.1904 mL 5.4760 mL
25 mM 0.1752 mL 0.8762 mL 1.7523 mL 4.3808 mL
30 mM 0.1460 mL 0.7301 mL 1.4603 mL 3.6506 mL
40 mM 0.1095 mL 0.5476 mL 1.0952 mL 2.7380 mL
50 mM 0.0876 mL 0.4381 mL 0.8762 mL 2.1904 mL
60 mM 0.0730 mL 0.3651 mL 0.7301 mL 1.8253 mL
80 mM 0.0548 mL 0.2738 mL 0.5476 mL 1.3690 mL
100 mM 0.0438 mL 0.2190 mL 0.4381 mL 1.0952 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    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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Agmatine sulfate
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