| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g | |||
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| Targets |
Pyridoxylamine targets reactive carbonyl species and advanced glycation end-product (AGE) formation. It is an effective scavenger of reactive carbonyls, preventing the late stages of glycation processes that lead to AGE formation. It also acts as a lipoxidation end products (ALEs) inhibitor. By inhibiting AGE and ALE formation, it reduces protein crosslinking and oxidative stress, protecting against diabetic complications.
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| ln Vitro |
Pyridoxylamine (PM), a B6 vitamer, is an effective scavenger of reactive carbonyls, preventing the late stages of glycation processes that result in AGE formation[1].
In vitro, Pyridoxylamine is an effective scavenger of reactive carbonyls, preventing the late stages of glycation processes. It inhibits the formation of advanced glycation end-products (AGEs). It is a potent inhibitor of AGEs and ALEs. These activities have been demonstrated in various in vitro models of glycation and oxidative stress. Quantitative IC50 values for its effects are not detailed in the publicly available sources. |
| ln Vivo |
Pyridoxylamine finally prevents the development of nephropathy in STZ-diabetic rats by limiting the production of CML and CEL as well as cross-linking in skin collagen. Since pyridoxylamine does not stop lipid peroxidation events, it does not seem to have an antioxidant effect. In addition, it inhibits the development of 4-hydroxynonenal adducts and malondialdehyde on protein in Zucker rats in vivo, which are results of lipid peroxidation that modify proteins[1].
In vivo, Pyridoxylamine has been shown to protect against diabetes-induced retinal vascular lesions. It inhibits the development of retinopathy in experimental diabetes. As a B6 vitamer, it plays a role in amino acid metabolism and functions as a coenzyme in transamination reactions. Its protective effects against glycation and oxidative stress make it a compound of interest for the treatment of diabetic complications and other age-related diseases. |
| Enzyme Assay |
For cell-free assays, the activity of Pyridoxylamine can be measured by assessing its ability to scavenge reactive carbonyl species, such as methylglyoxal or glyoxal, using HPLC or mass spectrometry. Its inhibition of AGE formation can be assessed by incubating the compound with a protein (e.g., BSA) and a glycating agent (e.g., glucose or ribose), and measuring the formation of fluorescent AGEs or specific AGE adducts (e.g., carboxymethyllysine) by ELISA or LC-MS.
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| Cell Assay |
For in vitro cellular assays, the protective effects of Pyridoxylamine can be assessed in cell culture models of glycation and oxidative stress. Cells (e.g., endothelial cells, retinal cells) are treated with glycating agents and/or oxidative stressors in the presence and absence of Pyridoxylamine. Endpoints include cell viability, ROS production, AGE formation, and expression of inflammatory markers. Its effect on cellular metabolism can also be assessed.
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| Animal Protocol |
For in vivo studies, Pyridoxylamine is typically administered orally or intraperitoneally in animal models of diabetes, such as streptozotocin-induced diabetic rats or mice. Endpoints include blood glucose levels, HbA1c, AGE levels in tissues (e.g., retina, kidney), and markers of oxidative stress and inflammation. Its protective effects on diabetic complications, such as retinopathy and nephropathy, can be assessed by histology and functional tests.
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| ADME/Pharmacokinetics |
Pyridoxylamine (CAS 85-87-0) has a molecular formula of C8H12N2O2 and a molecular weight of 168.19 g/mol. Its IUPAC name is 4-(aminomethyl)-5-(hydroxymethyl)-2-methylpyridin-3-ol. Appearance: White to yellow solid. Solubility: DMSO: 16.67 mg/mL (99.11 mM). Storage: typical for vitamins (desiccated, protected from light). Purity: typically ≥95% for research use.
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| Toxicity/Toxicokinetics |
No detailed toxicity data is publicly available. As a vitamin B6 derivative, it is generally considered safe at physiological and nutritional doses. It is a natural metabolite and is generally recognized as safe. High doses may cause neurological side effects, similar to other B6 vitamers. Standard toxicological studies would be required for therapeutic development at higher doses.
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| References | |
| Additional Infomation |
Pyridoxamine is a monohydroxypyridine with a pyridine ring structure, where a hydroxyl group is substituted at position 3, an aminomethyl group at position 4, a hydroxymethyl group at position 5, and a methyl group at position 2. It is the 4-aminomethyl form of vitamin B6 and is used in the form of hydrochloride to treat diabetic nephropathy. Pyridoxamine is metabolized in humans, Saccharomyces cerevisiae, Escherichia coli, plants, and mice, and acts as an iron chelating agent and nephroprotective agent. It is a hydroxymethylpyridine, monohydroxypyridine, aminoalkylpyridine, and vitamin B6. It is the conjugate base of Pyridoxamine (1+). Pyridoxamine has been used in clinical trials for the treatment of kidney stones. Pyridoxamine is a metabolite found or produced in Escherichia coli (K12 strain, MG1655 strain). Pyridoxamine has also been reported in soybeans, fruit flies, and other organisms with relevant data. It is the 4-aminomethyl form of vitamin B6. During amino acid transamination, pyridoxal phosphate is transiently converted to Pyridoxamine phosphate.
Pyridoxylamine is a research-grade compound and is not approved as a drug in the United States. It is a vitamin B6 derivative and a potent inhibitor of AGE formation. Its mechanism of action involves scavenging reactive carbonyl species and inhibiting AGE formation. It has been studied for its potential to treat diabetic complications. No clinical trials have been reported for this specific compound, but it has been studied in preclinical models. |
| Molecular Formula |
C₈H₁₂N₂O₂
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| Molecular Weight |
168.19
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| Exact Mass |
168.09
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| CAS # |
85-87-0
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| PubChem CID |
1052
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| Appearance |
White to yellow solid powder
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| Density |
1.282g/cm3
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| Boiling Point |
460.1ºC at 760 mmHg
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| Flash Point |
232.1ºC
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| Index of Refraction |
1.617
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| LogP |
0.746
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
12
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| Complexity |
143
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
NHZMQXZHNVQTQA-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C8H12N2O2/c1-5-8(12)7(2-9)6(4-11)3-10-5/h3,11-12H,2,4,9H2,1H3
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| Chemical Name |
4-(aminomethyl)-5-(hydroxymethyl)-2-methylpyridin-3-ol
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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 |
| 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) |
DMSO : ~16.67 mg/mL (~99.11 mM)
H2O : ~6.25 mg/mL (~37.16 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (12.37 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (12.37 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (12.37 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 5.9457 mL | 29.7283 mL | 59.4566 mL | |
| 5 mM | 1.1891 mL | 5.9457 mL | 11.8913 mL | |
| 10 mM | 0.5946 mL | 2.9728 mL | 5.9457 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.
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