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500mg |
ln Vitro |
In L02 cells, KEAP1-Nrf2-IN-1 (compound 35) concentration-dependently raises the mRNA levels of the Nrf2 regulatory genes NEFL2L (encoding Nrf2 protein), HO-1, NQO-1, and GCLM [1]. Keap1-Nrf2-IN-1 (0.1-10 μM; 12 hours) increases Nrf2, heme oxygen-1 (HO-1), NAD (P) H dehydrogenase (quinone) in L02 cells 1 (NQO-1) and glutamate-cysteine ligase regulatory subunit (GCLM) protein levels in a concentration-dependent manner [1]. Acetaminophen-induced L02 cell damage is protected against by the cytoprotective actions of Keap1-Nrf2-IN-1 (1 – 20 μM; 12 hours) [1].
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ln Vivo |
In an in vivo model, acetaminophen-induced liver injury is countered by Keap1-Nrf2-IN-1 (40 mg/kg; i.p.) [1].
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Cell Assay |
Western Blot Analysis[1]
Cell Types: L02 cells Tested Concentrations: 0.1 μM, 1 μM, 5 μM, 10 μM Incubation Duration: 12 hrs (hours) Experimental Results: Up-regulated the protein levels of Nrf2 and Nrf2 downstream proteins. |
Animal Protocol |
Animal/Disease Models: 6-8 weeks female C57BL/6 mice (18-20 g)[1]
Doses: 40 mg/kg Route of Administration: intraperitoneal (ip)injection Experimental Results: Ameliorated the pathological symptoms in the Acetaminophen (400 mg/kg; ip)-induced mouse model of acute liver injury. |
References |
[1]. Lu MC, et al. Discovery of a Potent Kelch-Like ECH-Associated Protein 1-Nuclear Factor Erythroid 2-Related Factor 2 (Keap1-Nrf2) Protein-Protein Interaction Inhibitor with Natural Proline Structure as a Cytoprotective Agent against Acetaminophen-Induced Hepatotoxicity. J Med Chem. 2019 Jul 25;62(14):6796-6813.
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Molecular Weight |
0
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CAS # |
2232112-72-8
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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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) |
DMSO : ~100 mg/mL (~206.39 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 4.55 mg/mL (9.39 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 45.5 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. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.16 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.16 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
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.