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| Targets |
MJ33 lithium salt targets the acidic, calcium-independent (ai)PLA2 activity of peroxiredoxin 6 (Prdx6), a bifunctional enzyme that also possesses non-selenium glutathione peroxidase activity. By inhibiting the iPLA2 activity of Prdx6, MJ33 lithium salt interferes with the enzyme's role in phospholipid metabolism and ROS production.
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| ln Vitro |
In vitro, MJ33 lithium salt selectively suppresses the aiPLA2 activity of both recombinant and native Prdx6 by binding to the enzyme's catalytic site. It inhibits phosphorylation-stimulated Prdx6 activity, demonstrating its competitive and reversible mechanism. The compound is often used to dissect the specific role of Prdx6-mediated PLA2 activity in cellular models of oxidative stress and inflammation.
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| ln Vivo |
In vivo, MJ33 lithium salt has been studied for its effects in acute lung injury models, where inhibition of Prdx6 aiPLA2 activity reduces lung inflammation and injury. By blocking the PLA2 activity of Prdx6, it modulates pulmonary surfactant degradation and inflammatory signaling pathways. MJ33 lithium salt is typically administered via intraperitoneal injection in rodent models to evaluate its therapeutic potential in respiratory diseases.
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| Enzyme Assay |
To assess MJ33 lithium salt as an aiPLA2 inhibitor, recombinant human Prdx6 protein is incubated with varying concentrations of MJ33 in reaction buffer containing 1-palmitoyl-2-[14C]arachidonoyl-sn-glycero-3-phosphocholine as substrate. Reactions are terminated after a set time (typically 30-60 minutes) by addition of organic solvent. Radioactive products are extracted and quantified by liquid scintillation counting to calculate IC50 values.
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| Cell Assay |
For in vitro cell assays, cells such as A549 lung epithelial cells are pretreated with escalating concentrations of MJ33 lithium salt for 1-2 hours. Cells are then stimulated with agents that induce ROS generation or PLA2 activation. After incubation, markers of oxidative stress (e.g., ROS levels), phospholipase activity, or inflammatory cytokine production are measured. Cytotoxicity is assessed using MTT or LDH assays to determine non-toxic concentration ranges.
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| Animal Protocol |
In rodent models, MJ33 lithium salt is typically administered via intraperitoneal injection at doses ranging from 1-20 mg/kg in saline or DMSO:PBS vehicle. To study acute lung injury, mice are challenged with lipopolysaccharide (LPS) or other inflammatory stimuli, and MJ33 treatment is given before or after challenge. Bronchoalveolar lavage fluid (BALF) is collected to measure inflammatory cells, protein levels, and cytokine concentrations. Lung tissue is harvested for histology and biochemical analysis.
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| ADME/Pharmacokinetics |
Systematic pharmacokinetic studies for MJ33 lithium salt are limited. Based on structural properties as a phospholipid analog, MJ33 is expected to distribute into lipid-rich tissues. The compound is typically formulated in saline with or without DMSO and administered via intraperitoneal injection. Bioavailability and elimination half-life in rodent models have not been extensively characterized; researchers should conduct pilot PK studies for their specific experimental conditions.
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| Toxicity/Toxicokinetics |
Available toxicological data for MJ33 lithium salt is limited. In cell-based assays, MJ33 shows low cytotoxicity at concentrations used for aiPLA2 inhibition (typically ≤50 uM). In animal studies at therapeutic doses (e.g., 5-10 mg/kg i.p.), no major acute toxicity or behavioral abnormalities have been reported. However, comprehensive toxicology studies including repeated-dose toxicity and organ-specific safety assessments have not been published. Researchers should conduct appropriate toxicity controls for their models.
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| References | |
| Additional Infomation |
MJ33 lithium salt is a research tool compound and is not approved for clinical use. It has no ongoing clinical trials or approved indications. The compound acts by competitively binding to the active site of Prdx6's aiPLA2 domain, blocking its phospholipase activity without affecting its peroxidase function. This selectivity makes MJ33 valuable for dissecting the independent roles of Prdx6's two enzymatic activities. The compound is sensitive to moisture and should be stored at -20degC in sealed containers.
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| Molecular Formula |
C22H43F3LIO6P
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| Molecular Weight |
498.48
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| Exact Mass |
498.29
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| CAS # |
1007476-63-2
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| PubChem CID |
4214
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
23
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| Heavy Atom Count |
33
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| Complexity |
472
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| Defined Atom Stereocenter Count |
0
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| SMILES |
[Li+].CCCCCCCCCCCCCCCCOCC(COCC(F)(F)F)OP(=O)([O-])OC
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| InChi Key |
GDLMLQJISATCEL-UHFFFAOYSA-M
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| InChi Code |
InChI=1S/C22H44F3O6P.Li/c1-3-4-5-6-7-8-9-10-11-12-13-14-15-16-17-29-18-21(31-32(26,27)28-2)19-30-20-22(23,24)25;/h21H,3-20H2,1-2H3,(H,26,27);/q;+1/p-1
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| Chemical Name |
lithium;[1-hexadecoxy-3-(2,2,2-trifluoroethoxy)propan-2-yl] methyl phosphate
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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 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.) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0061 mL | 10.0305 mL | 20.0610 mL | |
| 5 mM | 0.4012 mL | 2.0061 mL | 4.0122 mL | |
| 10 mM | 0.2006 mL | 1.0030 mL | 2.0061 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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