Size | Price | Stock | Qty |
---|---|---|---|
500mg |
|
||
1g |
|
||
5g |
|
||
Other Sizes |
|
ln Vitro |
After promoting osteogenesis, apocynin (100 μM, 1-7, 14 days) dramatically raises the expression levels of osteogenic markers in aging BMSC cells [3]. Apocynin (1, 10, 100 μM; 48 hours) specifically prevents fibronectin staining and vH-ras-transfected 3Y1 cell proliferation [4]. Apocynin (1, 10, 100 μM; 3, 6, 12 hours) inhibits 3Y1 and HR-3Y1-2 cell growth.
|
---|---|
ln Vivo |
In SAMP6 samples, apocynin (0.1 mg/kg/day, intraperitoneally, three times a week for three months) enhanced bone mass and density [3]. Apocynin injection intraperitoneally (5 mg/kg)
|
Cell Assay |
Western Blot analysis [3]
Cell Types: Bone marrow stromal cells (BMSCs) Tested Concentrations: 100 μM Incubation Duration: 1-7, 14 days Experimental Results: Increased intracellular reactive oxygen species (ROS) levels [4]. "Dry Markers" Nanog and Oct-4. Reduces the expression levels of p53, p21 and p16 at both the mRNA and protein levels. Compared with the negative control group, the expressions of sox-2 and klf-4 increased by 82.4% and 38.7%, respectively. Compared with the negative control, the expression of NADPH oxidase was diminished by 66.5%. There were no changes in cell cycle or proliferation. The percentage of DSA-β-gal positive (green staining) cells was diminished by 42.5%. Increased expression levels of four key osteogenic markers (Runx2, OSX, Ocn, and Col1). Cell proliferation experiment [4] Cell Types: HR-3Y1-2, 3Y1 Cell Tested Concentrations: 0, 1, 10 or 100 μM Incubation Duration: 48 hrs (hours) Experimental Results: 10 μM inhibited HR-3Y1-2 cell proliferation, but not 3Y1 cells Proliferate 100 μM. RT-PCR[3] Cell Types: HR-3Y1-2, 3Y1 cells Tested Concentrations: 0, 1, 10, or 100 μM Incubation Duration: 24, 36, 48 h Experimental Results: Selectively down-regulated 1-integrin cell surface expression on the HR-3Y1-2 cells. diminished adhesion of HR-3Y1-2 cells to fibronectin-coated plates. |
Animal Protocol |
Animal/Disease Models: SAMP6 mouse model (pharmacokinetic/PK/PK determination) [3]
Doses: 0.1 mg/kg/day Route of Administration: intraperitoneal (ip) injection, weekly 3 times for 3 months. Experimental Results: Compared with the control group, the bone value was higher and the percentage of SA-β-gal positive cells was lower. The expression of Ki67 and Oct-4 mRNA was increased. Changes the osteoblast-osteoclast balance in bone and promotes osteoblast activity. Animal/Disease Models: Carrageenan induced pleurisy in male adult CD1 mice [5] Doses: 5 mg/kg Route of Administration: intraperitoneal (ip) injection Experimental Results: Blocked NADPH oxidase activation and attenuated neutrophils in lung tissue Cellular infiltration and lipid peroxidation. Reduce PARP activation and IL-1b expression. Prevents carrageenan-induced IkB-a degradation and reduces NF-kB p65 levels. Attenuate iNOS expression and reduce the degree of positive staining of Fas ligand in lung tissue. Inhibition of apoptosis in carrageenan-treated mice. Blocks Bax expression and r |
References |
[1]. Stefanska J, et al. Mediators Inflamm, 2008, 106507.
[2]. Stolk J,et al. Am J Respir Cell Mol Biol, 1994, 11(1), 95-102. [3]. Sun J, et.al. Apocynin suppression of NADPH oxidase reverses the aging process in mesenchymal stem cells to promote osteogenesis and increase bone mass. Sci Rep. 2015 Dec 21;5:18572. [4]. Yamasaki M, et.al. Selective inhibition by apocynin of the proliferation and adhesion to fibronectin of v-H-ras-transformed 3Y1 cells. Biosci Biotechnol Biochem. 2012;76(6):1177-81. [5]. Impellizzeri D et al. Effect of apocynin, a NADPH oxidase inhibitor, on acute lung inflammation. Biochem Pharmacol. 2011 Mar 1;81(5):636-48. |
Molecular Formula |
C9H10O3
|
---|---|
Molecular Weight |
166.18
|
Exact Mass |
166.063
|
CAS # |
498-02-2
|
Related CAS # |
Apocynin-d3;80404-23-5
|
Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
|
SMILES |
O(C([H])([H])[H])C1=C(C([H])=C([H])C(C(C([H])([H])[H])=O)=C1[H])O[H]
|
Synonyms |
Acetovanillone NSC-209524 NSC 209524
|
HS Tariff Code |
2934.99.9001
|
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)
|
Solubility (In Vitro) |
DMSO : ≥ 100 mg/mL (~601.79 mM)
H2O : ~3.33 mg/mL (~20.04 mM) |
---|---|
Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (15.04 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 (15.04 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 (15.04 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 | 6.0176 mL | 30.0879 mL | 60.1757 mL | |
5 mM | 1.2035 mL | 6.0176 mL | 12.0351 mL | |
10 mM | 0.6018 mL | 3.0088 mL | 6.0176 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.