| Size | Price | Stock | Qty |
|---|---|---|---|
| 10g |
|
||
| 25g |
|
||
| 50g |
|
||
| 100g |
|
||
| Other Sizes |
| Targets |
Methyl pyruvate can be metabolized to pyruvate, which enters the tricarboxylic acid (TCA) cycle and supports ATP production. It may act as an antioxidant by scavenging hydrogen peroxide and as an inhibitor of the mitochondrial permeability transition pore (mPTP). It also serves as a substrate for alanine aminotransferase and lactate dehydrogenase. No specific high-affinity receptor target is known.
|
|---|---|
| ln Vitro |
In vitro, methyl pyruvate (0.1-10 mM) protects primary neurons against glutamate-induced excitotoxicity (improves viability from 40% to 80% at 1 mM). It also reduces ROS production in mitochondria. It increases ATP levels in energy-depleted cells. It is a substrate for pyruvate kinase (Km ~0.5 mM). It has no direct cytotoxicity up to 20 mM. It is also used as a carbon source in bacterial culture.
|
| ln Vivo |
In vivo, methyl pyruvate has been studied in rat models of stroke and traumatic brain injury. Intraperitoneal administration of 500 mg/kg immediately after middle cerebral artery occlusion reduced infarct volume by 40% and improved neurological scores. In a rat model of cardiac arrest, administration of 1 g/kg IV improved survival and neurological outcome. It is rapidly metabolized to pyruvate and methanol.
|
| Enzyme Assay |
A pyruvate kinase activity assay: The enzyme (1 U) is incubated with 5 mM methyl pyruvate, 1 mM ADP, and 0.1 mM NADH in the presence of lactate dehydrogenase (2 U). The decrease in NADH absorbance at 340 nm is monitored for 5 min. The specific activity is calculated. For mPTP inhibition, isolated rat liver mitochondria are incubated with 200 uM CaCl2 to induce swelling, and methyl pyruvate (1-10 mM) is added; swelling is measured by decrease in absorbance at 540 nm.
|
| Cell Assay |
Primary rat cortical neurons are cultured in 96-well plates. Excitotoxicity is induced by 100 uM glutamate for 1 hour. Methyl pyruvate (0.1-10 mM) is added before, during, or after glutamate exposure. After 24 hours, cell viability is measured by LDH release or MTT. Methyl pyruvate at 1 mM significantly reduces LDH release (from 80% to 40%). ROS is measured using DCFH-DA; methyl pyruvate reduces fluorescence by 50% at 5 mM.
|
| Animal Protocol |
A rat middle cerebral artery occlusion (MCAO) model: male SD rats (n=10/group) undergo 2 hours of MCAO followed by 22 hours of reperfusion. Methyl pyruvate (500 mg/kg) is administered intraperitoneally immediately after reperfusion. Neurological deficit scores are assessed at 24 hours. The rats are then euthanized, and brain sections are stained with TTC to measure infarct volume. The treatment group shows reduced infarct volume by 40% compared to saline control.
|
| ADME/Pharmacokinetics |
Methyl pyruvate (MW 104.10, logP ~0.5) is rapidly absorbed after IP or IV administration. It is quickly hydrolyzed by plasma esterases to pyruvic acid and methanol. The half-life of the intact ester is <5 minutes. Pyruvate is then converted to lactate or enters the TCA cycle. The methanol released is metabolized to formaldehyde and formate, which at high doses can cause toxicity. The plasma half-life of total pyruvate equivalents is 30-60 minutes. The compound is cleared by metabolism.
|
| Toxicity/Toxicokinetics |
Acute toxicity: LD50 in mice is approximately 3-5 g/kg IP. The methanol byproduct may contribute to metabolic acidosis at very high doses (>1 g/kg). At therapeutic doses (500 mg/kg), no significant toxicity is observed. The compound is a mild skin and eye irritant. Not a mutagen. Not a carcinogen. Standard laboratory safety: gloves, goggles. The compound is stable at room temperature.
|
| References |
|
| Additional Infomation |
Methyl pyruvate is a pyruvate ester formed by the condensation of the carboxyl group of pyruvate and the hydroxyl group of methanol. It is both a methyl ester and a pyruvate ester, and functionally related to pyruvate. Methyl pyruvate has been reported in the genus *Peristeria elata*, and relevant data are available for reference.
Methyl pyruvate is a research chemical used to study energy metabolism and as a neuroprotective agent in preclinical models. It has been explored as a potential treatment for ischemic stroke, traumatic brain injury, and Parkinson's disease, but has not advanced to clinical trials. It is also used as a flavoring agent and as a building block in organic synthesis. The mechanism of neuroprotection is thought to involve increasing cellular ATP, reducing ROS, and inhibiting the mitochondrial permeability transition. The compound is not an FDA-approved drug. No Phase 3 trials have been reported. |
| Molecular Formula |
C4H6O3
|
|---|---|
| Molecular Weight |
102.09
|
| Exact Mass |
102.032
|
| CAS # |
600-22-6
|
| PubChem CID |
11748
|
| Appearance |
Colorless to light yellow liquid
|
| Hydrogen Bond Donor Count |
0
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
7
|
| Complexity |
95.1
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CC(=O)C(=O)OC
|
| InChi Key |
CWKLZLBVOJRSOM-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C4H6O3/c1-3(5)4(6)7-2/h1-2H3
|
| Chemical Name |
methyl 2-oxopropanoate
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ~200 mg/mL (~1959.06 mM; with sonication)
|
|---|---|
| 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 | 9.7953 mL | 48.9764 mL | 97.9528 mL | |
| 5 mM | 1.9591 mL | 9.7953 mL | 19.5906 mL | |
| 10 mM | 0.9795 mL | 4.8976 mL | 9.7953 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
