| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
TLR4/NF-κB-IN-2 (compound G-12) (5 μM; pre-incubation for 1 h, LPS stimulation for 24 h) effectively inhibited LPS-induced NO production in BV2 cells, with an IC50 value of 1.39 ± 0.11 μM [1]. TLR4/NF-κB-IN-2 (2.5-10 μM; pre-incubation for 3 h, H2O2 exposure for 24 h) effectively protected PC12 cells from H2O2-induced cell death, with an IC50 value of 1.29 ± 0.02 μM, and increased cell viability in a concentration-dependent manner [1]. TLR4/NF-κB-IN-2 (2.5-10 μM; pre-incubation for 2 h, LPS stimulation for 6 h) reduced LPS-induced intracellular ROS accumulation in BV2 cells in a dose-dependent manner [1]. TLR4/NF-κB-IN-2 (2.5-10 μM; pre-incubation for 2 hours, LPS stimulation for 24 hours) can activate the Nrf2/HO-1 signaling pathway in LPS-stimulated BV2 cells, enhancing Nrf2 nuclear translocation and HO-1 expression in a concentration-dependent manner [1]. TLR4/NF-κB-IN-2 (2.5-10 μM; pre-incubation for 2 hours, LPS stimulation for 24 hours) can inhibit the TLR4/NF-κB signaling pathway in LPS-induced BV2 cells, reducing TLR4 expression and the phosphorylation levels of downstream IκBα and p65 in a concentration-dependent manner [1].
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| ln Vivo |
TLR4/NF-κB-IN-2 (compound G-12) (2.5-10 mg/kg; orally; once daily for 7 days) can dose-dependently improve cognitive function, reduce the accumulation of Aβ1-42, protect hippocampal neurons, inhibit glial cell activation and neuroinflammation, and alleviate oxidative stress in Aβ1-42-induced Alzheimer's disease model mice [1].
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| Cell Assay |
Cell viability assay [1]
Cell Types: PC12 rat pheochromocytoma cells Tested Concentrations: 2.5, 5 and 10 μM Incubation Duration: 3 hours (pre-incubation); 24 hours (H2O2 treatment) Experimental Results: The viability of PC12 cells treated with H2O2 increased from 50.66% to 73.85% (2.5 μM), 86.92% (5 μM) and 94.16% (10 μM). It had a protective effect against H2O2-induced cell death, with an IC50 value of 1.29 μM. Western Blot Analysis [1] Cell Types: BV2 mouse microglia Tested Concentrations: 2.5, 5, and 10 μM Incubation Duration: 2 hours (pre-incubation); 24 hours (LPS stimulation) Experimental Results: LPS-induced Nrf2 nuclear translocation was enhanced in a concentration-dependent manner. HO-1 protein expression increased in a concentration-dependent manner, with the HO-1/β-actin ratio increasing from ~0.8 (LPS only) to approximately 1.0 (2.5 μM), ~1.0 (5 μM), and ~1.2 (10 μM). LPS-induced TLR4 protein expression decreased in a concentration-dependent manner, with the TLR4/β-actin ratio decreasing from ~1.0 (LPS only) to approximately 0.5 (10 μM). IκBα phosphorylation levels decreased in a concentration-dependent manner, with the P-IκBα/IκBα ratio decreasing from ~1.1 (LPS group only) to approximately 0.8 (10 μM). p65 phosphorylation levels also decreased in a concentration-dependent manner, with the P-p65/p65 ratio decreasing from ~1.1 (LPS group only) to approximately 0.7 (10 μM). |
| Animal Protocol |
Animal/Disease Models:ICR mice (male, 6-8 weeks old, 18-25 g, induced by intraventricular injection of Aβ1-42 peptide)[1]
Doses: 2.5 mg/kg; 10 mg/kg Route of Administration: Oral; once daily for 7 days Experimental Results: Reversed the reduction in total movement distance, average speed and central region movement distance in the Aβ1-42-induced open field test. In a 5-day Morris water maze training, it shortened the escape latency, increased the number of platform crossings, and increased the time spent in the target quadrant in the probe test. Hippocampal Aβ1-42 concentrations decreased from approximately 70 μg/L to approximately 60 μg/L (2.5 mg/kg) and approximately 48 μg/L (10 mg/kg); whole-brain Aβ1-42 concentrations decreased from approximately 42 μg/L to approximately 38 μg/L (2.5 mg/kg) and approximately 31 μg/L (10 mg/kg). The number of neurons in the hippocampal dentate gyrus (DG), CA1, and CA3 regions increased; at a dose of 10 mg/kg, the number of DG neurons increased from approximately 240 to approximately 460, and the number of CA1 neurons increased from approximately 80 to approximately 150. A dose-dependent reduction in the percentage of GFAP-positive astrocytes and Iba-1-positive microglia in the hippocampus was observed, causing glial cells to transition from a reactive to a resting morphology. Hippocampal TNF-α levels decreased from approximately 185 pg/mL to approximately 148 pg/mL (2.5 mg/kg) and approximately 105 pg/mL (10 mg/kg); IL-6 levels decreased from approximately 228 pg/mL to approximately 165 pg/mL (2.5 mg/kg) and approximately 135 pg/mL (10 mg/kg); hippocampal MDA levels decreased from approximately 180 nmol/mg protein to approximately 165 nmol/mg protein (2.5 mg/kg) and approximately 120 nmol/mg protein (10 mg/kg); SOD activity increased from approximately 2.8 U/mg protein to approximately 3.8 U/mg protein (2.5 mg/kg) and approximately 4.2 U/mg protein (10 mg/kg). |
| References |
| Molecular Formula |
C27H32FNO3
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|---|---|
| Molecular Weight |
437.55
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| Appearance |
Typically exists as solids at room temperature
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| SMILES |
O=C(C(O)=C1[C@@H]2C=C(C)CC[C@H]2C(C)=C)C(CCCCC)=C(NC3=CC=C(F)C=C3)C1=O
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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 | 2.2855 mL | 11.4273 mL | 22.8545 mL | |
| 5 mM | 0.4571 mL | 2.2855 mL | 4.5709 mL | |
| 10 mM | 0.2285 mL | 1.1427 mL | 2.2855 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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