| Size | Price | Stock | Qty |
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| 10g |
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| 25g |
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| 50g |
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| 100g |
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| 200g |
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| Other Sizes |
| Targets |
Methylthioninium chloride hydrate targets multiple enzymes: guanylyl cyclase (sGC), monoamine oxidase A (MAO-A), and nitric oxide synthase (NOS). By inhibiting sGC and NOS, it reduces NO-cGMP signaling pathways. Inhibition of MAO-A affects monoamine neurotransmitter metabolism. The compound is a redox cycling compound capable of generating reactive oxygen species and modulating cellular redox balance. It crosses the blood-brain barrier and has been studied for neuroprotective effects. As a vasopressor, it restores vascular tone and normalizes mean arterial pressure.
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| ln Vitro |
Methylene Blue (1, 5, and 25 μg/rat) significantly reduces brain cyclic guanosine monophosphate (cGMP) content and sevoflurane minimum alveolar anesthetic concentration (MAC) in a dose-dependent manner in male Sprague-Dawley rats (7-week-old, 200-250 g)[2]. Methylene blue is used as a dye in chromoendoscopy, and is sprayed onto the mucosa of the gastrointestinal tract in order to identify dysplasia, or pre-cancerous lesions[2]. Methylene blue is able to restore vascular tone, normalize mean arterial pressures (MAP), and reduce vasopressor usage[3].
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| ln Vivo |
Methylene Blue (1, 5, and 25 μg/rat) significantly reduces brain cyclic guanosine monophosphate (cGMP) content and sevoflurane minimum alveolar anesthetic concentration (MAC) in a dose-dependent manner in male Sprague-Dawley rats (7-week-old, 200-250 g)[2]. Methylene blue is sprayed onto the gastrointestinal tract mucosa during chromoendoscopy as a dye to detect dysplasia, or precancerous lesions[2]. Methylene blue has the power to lower the need for vasopressors, normalize mean arterial pressures (MAP), and restore vascular tone[3]. |
| Enzyme Assay |
In vitro enzyme/receptor binding studies for Methylthioninium chloride hydrate involve inhibition assays for sGC, MAO-A, and NOS. sGC activity is assessed by measuring cGMP production in the presence of increasing concentrations of the compound. MAO-A activity is measured using recombinant MAO-A incubated with a substrate such as kynuramine or serotonin, with product formation detected fluorometrically. NOS activity is assessed by monitoring the conversion of L-arginine to L-citrulline. IC50 values are calculated from dose-response curves. Standard protocols use purified enzymes or tissue homogenates.
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| Cell Assay |
In vitro cellular assays for Methylthioninium chloride hydrate involve culturing various cell types (neuronal, endothelial, cancer cells) in the presence of serial dilutions of the compound. Cell viability is assessed using MTT or resazurin assays. ROS production is measured using fluorescent probes such as DCFH-DA. Enzyme inhibition is assessed by measuring downstream products (e.g., cGMP for guanylate cyclase, monoamine levels for MAO-A). Neuroprotective effects are evaluated in models of oxidative stress or excitotoxicity. The compound's redox cycling properties are studied by measuring changes in cellular redox state.
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| Animal Protocol |
In vivo animal studies for Methylthioninium chloride hydrate include models of neurodegenerative diseases, methemoglobinemia, and vasoplegic shock. Animals are treated with the compound via intravenous, intraperitoneal, or oral administration. In rat studies, doses of 1, 5, and 25 μg/rat have been used to evaluate effects on brain cGMP content and sevoflurane MAC. Endpoints include behavioral tests, biochemical analysis of oxidative stress markers, histological examination, and physiological parameters (blood pressure, heart rate). Standard protocols include dose-response assessment and comparison to vehicle or reference treatments.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Methylthioninium chloride hydrate include good bioavailability and distribution, with the ability to cross the blood-brain barrier. The compound has a molecular formula of C₁₆H₂₄ClN₃O₃S and a molecular weight of 373.90. It is supplied as a solid powder. Methylene blue is rapidly absorbed and distributed throughout the body. It is metabolized in the liver by various enzymes, including N-demethylation to leukomethylene blue, and excreted primarily in urine. Its half-life is approximately 5-6 hours. It is available in both oral and intravenous formulations for clinical use.
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| Toxicity/Toxicokinetics |
Methylthioninium chloride hydrate is generally safe at therapeutic doses. Common side effects include blue-green discoloration of urine and skin, nausea, vomiting, and headache. At high doses, it can cause serotonin syndrome (due to MAO-A inhibition), hemolytic anemia in G6PD-deficient patients, and neurotoxicity. It is contraindicated in patients with G6PD deficiency. Overdose can cause severe methemoglobinemia, respiratory distress, and cardiac arrhythmias. Its use requires careful dosing and monitoring. Long-term safety data are available from its extensive clinical use as methylene blue.
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| References |
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| Additional Infomation |
Methylthioninium chloride hydrate is the hydrated form of methylene blue, a versatile compound with a long history of medical use. It is also known as Basic Blue 9, Tetramethylthionine chloride, and TRx-014. Its CAS number is 7220-79-3 (hydrate). It is used as a vasopressor, dye, and treatment for methemoglobinemia and neurodegenerative diseases. It is also used in chromoendoscopy to detect gastrointestinal lesions. Its multiple enzyme targets and ability to cross the blood-brain barrier have made it a subject of research in neurodegenerative diseases. It is available for research and clinical use.
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| Molecular Formula |
C16H24CLN3O3S
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| Molecular Weight |
373.896
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| Exact Mass |
373.12
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| Elemental Analysis |
C, 51.40; H, 6.47; Cl, 9.48; N, 11.24; O, 12.84; S, 8.57
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| Appearance |
Solid powder
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| InChi Key |
XQAXGZLFSSPBMK-UHFFFAOYSA-M
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| InChi Code |
InChI=1S/C16H18N3S.ClH.3H2O/c1-18(2)11-5-7-13-15(9-11)20-16-10-12(19(3)4)6-8-14(16)17-13;;;;/h5-10H,1-4H3;1H;3*1H2/q+1;;;;/p-1
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| Chemical Name |
3,7-bis(dimethylamino)phenothiazin-5-ium chloride trihydrate
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| Synonyms |
3,7-bis(Dimethylamino)phenazathionium chloride, Basic Blue 9, Tetramethylthionine chloride; Methylthioninium Chloride; Methylene blue; TRx-014
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6745 mL | 13.3726 mL | 26.7451 mL | |
| 5 mM | 0.5349 mL | 2.6745 mL | 5.3490 mL | |
| 10 mM | 0.2675 mL | 1.3373 mL | 2.6745 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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