| Size | Price | Stock | Qty |
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| 100mg |
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| 500mg |
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| 1g |
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| Other Sizes |
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| ln Vitro |
Agmatine stimulates the release of catecholamines from adrenal chromaffin cells via binding to imidazoline and α2-adrenergic receptors. There is arginine decarboxylase, its biosynthetic enzyme, in the brain. Agmatine, which is generated topically, functions as a neurotransmitter and is an endogenous agonist of imidazoline receptors as well as a non-catecholamine ligand for α2-adrenergic receptors [1]. The brain produces gabapentin, which is then stored in synaptic vesicles of neurons that are selectively localized, accumulated by uptake, released upon depolarization, and rendered inactive by the gabapentin enzyme. Agmatine causes the release of some peptide hormones and inhibits nitric oxide synthase [2]. Agmatine, or 4-(aminobutyl)guanidine, is created when arginine decarboxylase breaks down L-arginine. Agmatine is not a precursor of NO; rather, it is a competitive inhibitor of all NOS isoenzymes. Ki values for NOS I, NOS II, and NOS III are roughly 660 µM, 220 µM, and 7.5 mM, respectively [3]. Agmatine causes three times as much nitrite to be produced by endothelial cells as they do at rest. Agmatine has been seen to cause cytosolic calcium transients in endothelial cells and to displace [3H]-imidazoxane on the endothelial cell membrane. Agmatine downregulates transients when exposed repeatedly; transients are unaffected by norepinephrine pretreatment [4].
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| ln Vivo |
Agmatine has antidepressant-like effects when tested in mice using the forced swim test and tail suspension test (dose range: 0.01–50 mg/kg, intraperitoneally), but it does not affect the mice's ability to walk in the open [5]. Agmatine preserves the blood-brain barrier during ischemic stroke; this can be observed in vivo by measuring permeability with dynamic contrast-enhanced magnetic resonance imaging [6]. Agmatine notably increased MK-801's antidepressant-like effects, supporting the theory that it modifies NMDA receptor activity [7].
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| References |
| Molecular Formula |
C5H16N4O4S
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|---|---|
| Molecular Weight |
228.2699
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| Exact Mass |
228.089
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| CAS # |
2482-00-0
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| Related CAS # |
306-60-5 ( free base);2482-00-0 (sulfate);
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| PubChem CID |
2794990
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| Appearance |
White to off-white solid powder
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| Boiling Point |
281.4ºC at 760 mmHg
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| Melting Point |
234-238 °C(lit.)
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| Flash Point |
124ºC
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| Vapour Pressure |
0.00357mmHg at 25°C
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| LogP |
1.527
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
14
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| Complexity |
166
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
PTAYFGHRDOMJGC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C5H14N4.H2O4S/c6-3-1-2-4-9-5(7)8;1-5(2,3)4/h1-4,6H2,(H4,7,8,9);(H2,1,2,3,4)
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| Chemical Name |
2-(4-aminobutyl)guanidine;sulfuric acid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O : ≥ 100 mg/mL (~438.08 mM)
DMSO : ~1 mg/mL (~4.38 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 25 mg/mL (109.52 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with heating and sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.4381 mL | 2.1904 mL | 4.3808 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT01524666 | Unknown † | Peripheral Neuropathy | JFK Medical Center | February 2012 |
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