| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| Other Sizes |
Purity: ≥98%
| Targets |
U83836E targets lipid peroxidation, a process in which reactive oxygen species (ROS) attack polyunsaturated fatty acids in cell membranes, leading to oxidative damage and cell death. As a lipid peroxidation inhibitor, U83836E prevents the oxidative degradation of lipids and protects cells from oxidative stress-induced damage. The compound also activates protein kinase C (PKC), which may contribute to its neuroprotective effects. U83836E belongs to the lazaroid class of compounds, which are known for their antioxidant and neuroprotective properties. The compound's ability to inhibit lipid peroxidation and activate PKC makes it a valuable tool for studying oxidative stress and neuroprotection.
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| ln Vitro |
U83836E demonstrates potent in vitro activity as a lipid peroxidation inhibitor. The compound prevents hydrogen peroxide-induced F2 isoprostane production in renal proximal tubular cells, demonstrating its ability to protect cells from oxidative damage. U83836E also prevents free radical-mediated effects of oxyhemoglobin in vascular smooth muscle. The compound has anti-tumor activity and inhibits glioma cell proliferation. Additionally, U83836E inhibits tumor necrosis factor and reverses endotoxin-induced shock. These diverse activities are consistent with the compound's ability to inhibit lipid peroxidation and modulate inflammatory responses. The compound's neuroprotective activity has been demonstrated in various in vitro models of oxidative stress.
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| ln Vivo |
U83836E has demonstrated in vivo efficacy in models of oxidative stress and neurodegeneration. The compound reduces secondary brain injury in a rabbit model of cryogenic trauma. This finding confirms the neuroprotective potential of U83836E in the context of traumatic brain injury. The compound's ability to reverse endotoxin-induced shock further supports its anti-inflammatory and protective effects in vivo. U83836E has also been shown to have neuroprotective activity in models of diabetic retinopathy, where it suppresses oxidative stress and improves neurodegeneration. These in vivo findings support the utility of U83836E as a tool for studying oxidative stress, neuroprotection, and inflammation.
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| Enzyme Assay |
The in vitro lipid peroxidation inhibition assay for U83836E measures the compound's ability to prevent the oxidative degradation of lipids. Liposomes or cell membrane preparations are incubated with an oxidant (e.g., hydrogen peroxide, iron/ascorbate) in the presence of varying concentrations of U83836E (typically ranging from nanomolar to micromolar). Lipid peroxidation is monitored by measuring the production of malondialdehyde (MDA) or F2-isoprostanes using colorimetric, fluorometric, or chromatographic methods. The inhibition of lipid peroxidation is quantified, and IC50 values are determined by fitting dose-response curves to the inhibition data. The compound is dissolved in DMSO and diluted in assay buffer to achieve the desired final concentrations, with DMSO concentration kept constant across all wells. Appropriate positive controls (known antioxidants) and negative controls (DMSO vehicle) are included in each assay run.
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| Cell Assay |
The in vitro cellular assay for U83836E is performed using cells that are susceptible to oxidative stress, such as renal proximal tubular cells, vascular smooth muscle cells, or glioma cells. Cells are cultured in appropriate medium and treated with varying concentrations of U83836E or vehicle control (DMSO). Oxidative stress is induced by exposure to hydrogen peroxide, oxyhemoglobin, or other pro-oxidant stimuli. Cellular oxidative damage is assessed by measuring F2-isoprostane production, lipid peroxidation, or cell viability. The protective effects of U83836E against oxidative damage are quantified. Additionally, the compound's effects on cell proliferation (e.g., glioma cell proliferation) and inflammatory responses (e.g., TNF-α production) can be assessed. Dose-response relationships are established by analyzing the protective effects across different compound concentrations.
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| Animal Protocol |
In vivo animal experiments with U83836E have been conducted using a rabbit model of cryogenic trauma. In this model, brain injury is induced by applying a cold probe to the brain surface, leading to localized edema and secondary injury. U83836E is administered at various doses, and the extent of secondary brain injury is assessed by measuring edema, neuronal loss, and functional outcomes. The compound has also been evaluated in models of diabetic retinopathy and endotoxin-induced shock. In these models, U83836E is administered via appropriate routes (e.g., intraperitoneal, intravenous, or oral), and endpoints such as oxidative stress markers, inflammatory cytokines, and tissue damage are measured. The compound's neuroprotective, anti-inflammatory, and anti-tumor activities are evaluated in these models.
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| ADME/Pharmacokinetics |
Detailed pharmacokinetic (PK) parameters for U83836E are not extensively documented in publicly available sources. As a small-molecule lipid peroxidation inhibitor with a molecular weight of 593.63, the compound is expected to have moderate oral bioavailability. U83836E has a chemical formula of C30H46Cl2N6O2. The compound is soluble in DMSO for formulation purposes. For in vivo administration, U83836E is typically formulated using appropriate vehicles to ensure adequate solubility and stability. The compound should be stored under conditions recommended by the manufacturer to maintain stability and prevent degradation. Detailed PK parameters including half-life, clearance, volume of distribution, and maximum concentration (Cmax) are not available from the current search results and would require consultation of the primary literature.
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| Toxicity/Toxicokinetics |
Comprehensive toxicological data for U83836E are not extensively documented in publicly available sources. As a research-grade compound, U83836E is intended for laboratory research purposes only and is not approved for human therapeutic use. Standard laboratory safety practices should be followed when handling this compound, including the use of appropriate personal protective equipment and working in a well-ventilated area. The compound should be stored according to the manufacturer's recommendations to maintain stability and prevent degradation. In animal studies, U83836E has been reported to be tolerated at the doses tested for neuroprotection and anti-inflammatory activity. However, comprehensive toxicological profiling (e.g., LD50, maximum tolerated dose, organ-specific toxicity) is not available from the current search results and would require consultation of the primary literature or safety data sheets.
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| References |
Cell Chem Biol. 2017 Aug 17;24(8):1029-1039.e7.
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| Additional Infomation |
U83836E is a research compound developed for studying oxidative stress, neuroprotection, and inflammation. The compound is a potent lipid peroxidation inhibitor belonging to the lazaroid class. U83836E has demonstrated neuroprotective activity in models of traumatic brain injury and diabetic retinopathy, anti-tumor activity against glioma cells, and anti-inflammatory activity by inhibiting tumor necrosis factor and reversing endotoxin-induced shock. The compound prevents oxidative damage in various cell types and reduces secondary brain injury in vivo. U83836E is not currently in clinical trials nor approved for therapeutic use; it remains an investigational tool compound for preclinical research. The compound is available from various chemical suppliers for research purposes.
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| Molecular Formula |
C30H46CL2N6O2
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| Molecular Weight |
593.63100
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| Exact Mass |
592.305
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| CAS # |
137018-55-4
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| PubChem CID |
9808654
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
5.95
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
40
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| Complexity |
783
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| Defined Atom Stereocenter Count |
1
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| SMILES |
Cl[H].Cl[H].O1C2C(C([H])([H])[H])=C(C([H])([H])[H])C(=C(C([H])([H])[H])C=2C([H])([H])C([H])([H])[C@]1(C([H])([H])[H])C([H])([H])N1C([H])([H])C([H])([H])N(C2C([H])=C(N=C(N=2)N2C([H])([H])C([H])([H])C([H])([H])C2([H])[H])N2C([H])([H])C([H])([H])C([H])([H])C2([H])[H])C([H])([H])C1([H])[H])O[H]
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| InChi Key |
KJGXSMZHYBXPIS-ZHXNKHNVSA-N
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| InChi Code |
InChI=1S/C30H44N6O2.2ClH/c1-21-22(2)28-24(23(3)27(21)37)9-10-30(4,38-28)20-33-15-17-35(18-16-33)26-19-25(34-11-5-6-12-34)31-29(32-26)36-13-7-8-14-36;;/h19,37H,5-18,20H2,1-4H3;2*1H/t30-;;/m1../s1
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| Chemical Name |
(2R)-2-[[4-(2,6-Dipyrrolidin-1-ylpyrimidin-4-yl)piperazin-1-yl]methyl]-2,5,7,8-tetramethyl-3,4-dihydrochromen-6-ol;dihydrochloride
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| Synonyms |
U83836E; U-83836-E; U 83836 E; PNU-83836E; PNU 83836 E; PNU83836E; PNU 83836E;
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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 | 1.6846 mL | 8.4228 mL | 16.8455 mL | |
| 5 mM | 0.3369 mL | 1.6846 mL | 3.3691 mL | |
| 10 mM | 0.1685 mL | 0.8423 mL | 1.6846 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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