| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| ln Vitro |
HepG2 cell viability is strongly inhibited by methazine at concentrations of 100, 300, and 1000 µM [1]. HepG2 cells' energy metabolism is promoted to switch from aerobic tricarboxylic acid cycle (TCA) and oxidative phosphorylation to anaerobic glycolysis by methazine (3, 10, 30 µM; 24 h) [1]. In HepG2 cells, promethazine (3, 10, 30 µM; 24 h) suppresses Complex IV activity [1].
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| ln Vivo |
There is an accumulation of triclofenac (46.3, 139, 417 mg/kg; po; single) in the kidney (18.64%), brain (23.58%), stomach (21.94%), and liver (35.84%)[1]. Promethazine (46.3, 139, 417 mg/kg; po; single) elevates MDA levels in mice's liver and brain more than in any other organ[1].
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| Cell Assay |
RT-PCR[1]
Cell Types: HepG2 cells Tested Concentrations: 3, 10, 30 µM Incubation Duration: 24 h Experimental Results: Dramatically increased lactate dehydrogenase B (LDHB) levels when at 30 µM, and slightly increased 6-phosphofructo-2-kinase /fructose-2,6-biphosphatase 3 (PFKFB3). diminished ATP levels in a concentration-dependent manner to 91.3, 87.9 and 67.2% of the levels in the vehicle control under treatment with 3, 10 and 30 µM buprofezin, respectively. Dramatically increased the lactate levels. Immunofluorescence[1] Cell Types: HepG2 cells Tested Concentrations: 3, 10, 30 µM Incubation Duration: 24 h Experimental Results: Dramatically inhibited the activity of Complex IV to 82.2, 69.2 and 63.4% of the vehicle control levels following buprofezin treatment at 3, 10 and 30 µM, respectively. Cell Viability Assay[1] Cell Types: HepG2 cells Tested Concentrations: 3, 10, 30 µM Incubation Duration: 24 h Experimental Results: Dramatically increased the intracellular ROS levels in a concentrate-independent manner, and diminished mtDNA contents. |
| Animal Protocol |
Animal/Disease Models: Male C57BL/6 mice (6 to 8weeks old)[1].
Doses: 46.3, 139, 417 mg/kg Route of Administration: Oral administration; single Experimental Results: Tended to elevate the MDA level in all organs, and the most significant concentration-dependent increases were observed in the liver and brain. demonstrated the highest concentrations in the liver (35.84%) followed by the brain (23.58%), stomach (21.94%) and kidney (18.64%), while the levels in the mouse spleen and heart were below the limit of detection. |
| References |
[1]. Ji X, et al. Potential hepatic toxicity of buprofezin at sublethal concentrations: ROS-mediated conversion of energy metabolism. J Hazard Mater. 2016 Dec 15;320:176-186.
[2]. YoshioIzawa, et al. Inhibition of chitin biosynthesis by buprofezin analogs in relation to their activity controlling Nilaparvata lugens Stål. Pestic Biochem Physiol, 1985, 24(3): 343-347. |
| Molecular Formula |
C16H23N3OS
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|---|---|
| Molecular Weight |
305.44
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| CAS # |
69327-76-0
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| Related CAS # |
Buprofezin-d6;2140803-94-5
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| SMILES |
CC(C)N1/C(=N\C(C)(C)C)/SCN(C2=CC=CC=C2)C1=O
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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) |
DMSO: 100 mg/mL (327.40 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.18 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (8.18 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (8.18 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2740 mL | 16.3698 mL | 32.7397 mL | |
| 5 mM | 0.6548 mL | 3.2740 mL | 6.5479 mL | |
| 10 mM | 0.3274 mL | 1.6370 mL | 3.2740 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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