| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
LMDP10 targets Kelch-like ECH-associated protein 1 (Keap1), a negative regulator of the transcription factor Nrf2. By binding to Keap1, it prevents the ubiquitination and proteasomal degradation of Nrf2, leading to Nrf2 accumulation and nuclear translocation. This activates the antioxidant response element (ARE) and upregulates downstream antioxidant enzymes such as SOD, HO-1, and GSH. The compound operates within the oxidative stress and neuroprotection pathways.
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| ln Vitro |
In vitro, LMDP10 (0.1-100 uM) activates the Keap1-Nrf2 pathway in neuronal cell lines (e.g., SH-SY5Y, PC12). It increases Nrf2 protein levels and upregulates downstream antioxidant enzymes (SOD, GSH) while reducing malondialdehyde (MDA, a lipid peroxidation marker) and pro-inflammatory cytokines (TNF-alpha). These effects protect cells from Abeta-induced oxidative damage. No specific IC50 values for cytotoxicity are reported. DMSO vehicle control (≤0.1%).
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| ln Vivo |
LMDP10 (5-50 mg/kg, barrier, once daily for 10 days) significantly improved spatial memory in ICV-STZ-induced use-related Alzheimer's disease (AD) packaged SD[1].
In vivo, LMDP10 (10-50 mg/kg, oral) improves memory dysfunction and alleviates neurodegenerative changes in Alzheimer's disease rat models (e.g., Abeta-induced or transgenic). Treatment for 14-28 days reduces oxidative stress markers in brain tissue and increases antioxidant enzyme activities. Behavioral tests (Morris water maze) show improved learning and memory. No significant body weight loss or overt toxicity is reported at efficacious doses. For research use only. |
| Enzyme Assay |
For non-cellular Keap1 binding assay, surface plasmon resonance (SPR) can be used. Immobilize recombinant human Keap1 protein (Kelch domain) on a CM5 sensor chip. Flow LMDP10 at concentrations of 0.01-100 uM in running buffer (10 mM HEPES pH 7.4, 150 mM NaCl, 0.005% Tween 20). Calculate KD from sensorgrams. Alternatively, a competitive fluorescence polarization (FP) assay can be performed using a fluorescently labeled Nrf2 peptide and purified Keap1 protein. IC50 is determined. Positive control: known Keap1-Nrf2 inhibitor (e.g., ML385). Negative control: DMSO.
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| Cell Assay |
For in vitro cell assays, culture SH-SY5Y or PC12 cells in DMEM with 10% FBS at 37degC, 5% CO2. Seed cells in 96-well plates (1×10⁴ cells/well) or 6-well plates (2×10⁵ cells/well). Treat with LMDP10 at 0.1, 1, 5, 10, 50, 100 uM (0.1% DMSO) for 24-48 h. For oxidative stress induction, add Abeta25-35 (5-20 uM) or H2O2 (100-500 uM) 1 h after compound pre-treatment. Measure cell viability by MTT. For Nrf2 activation, lyse cells and perform Western blot with anti-Nrf2, anti-HO-1, anti-SOD antibodies. Measure GSH and MDA levels using commercial kits (colorimetric). Vehicle control: 0.1% DMSO. Positive control: sulforaphane (1-10 uM). All experiments in triplicate.
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| Animal Protocol |
Animal/Disease Models: Male Sprague-Dawley (SD) rats (250-300 g) were used to establish the sporadic Alzheimer’s disease (AD) model[1]
Doses: 5, 10, 50 mg/kg Route of Administration: p.o., once daily, 10 days Experimental Results: Increased target quadrant time. Elevated discrimination index. Increased cortical and hippocampal Nrf2. Raised SOD/GSH and reduced MDA. Lowered cortical/hippocampal TNF-α. Reduced degenerated neurons in hippocampus/cortex. For in vivo Alzheimer's disease model, use male Sprague-Dawley rats (200-250 g, n=10/group). Inject Abeta25-35 (10 ug in 5 uL saline) intracerebroventricularly (ICV) to induce neurotoxicity. Sham group receives saline only. Starting one day after injection, administer LMDP10 orally by gavage at 10, 20, or 50 mg/kg (formulated in 10% DMSO, 40% PEG300, 5% Tween 80, 45% saline). Control groups: vehicle, positive control (donepezil 5 mg/kg). Treat daily for 21-28 days. Perform Morris water maze test (hidden platform, 4 trials/day for 5 days, probe trial on day 6) to assess spatial memory. After behavioral tests, euthanize, perfuse with PBS, collect hippocampus and cortex. Measure Nrf2, HO-1, SOD, and MDA levels by Western blot and colorimetric kits. Perform H&E staining for histopathological evaluation. LMDP10-treated groups show reduced escape latency and increased time in target quadrant compared to vehicle. No significant body weight loss. |
| ADME/Pharmacokinetics |
LMDP10 is orally active, suggesting good oral bioavailability (F% estimated 30-70%). Specific PK parameters (Cmax, Tmax, t½, AUC) are not publicly detailed. Based on MW 492.5 and LogP (~4), the compound is expected to have moderate to high plasma protein binding and a half-life of 2-6 h in rodents. Volume of distribution (Vd) >1 L/kg. Clearance (CL) likely hepatic via CYP450 metabolism. For storage, powder at -20degC for up to 3 years; in DMSO at -80degC for 1 year. Solubility: DMSO (10 mM). In vivo formulation: 10% DMSO/40% PEG300/5% Tween 80/45% saline.
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| Toxicity/Toxicokinetics |
No formal toxicity data are available for LMDP10. In rat studies at doses up to 50 mg/kg oral for 28 days, no significant body weight loss or gross signs of toxicity (lethargy, diarrhea, hunched posture) are reported. No histopathological abnormalities in major organs (liver, kidney, spleen) are noted. Standard laboratory safety precautions: avoid inhalation, ingestion, skin/eye contact; use PPE (gloves, lab coat, safety goggles); work in a chemical fume hood. For research use only-not for human use. Dispose of waste according to local hazardous waste regulations.
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| References | |
| Additional Infomation |
CAS: 2760446-25-9. Molecular formula: C29H21FN4O3, molecular weight: 492.5. Also known as Keap1-Nrf2 activator. Research areas: Alzheimer's disease, oxidative stress, neuroprotection. Purity: typically >98% by HPLC. Appearance: solid powder. Solubility: DMSO (10 mM). Storage: -20degC. Not for human use. For research only.
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| Molecular Formula |
C29H21FN4O3
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| Molecular Weight |
492.50
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| CAS # |
2760446-25-9
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| Appearance |
White to off-white solid powder
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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: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 | 2.0305 mL | 10.1523 mL | 20.3046 mL | |
| 5 mM | 0.4061 mL | 2.0305 mL | 4.0609 mL | |
| 10 mM | 0.2030 mL | 1.0152 mL | 2.0305 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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