| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
7,4'-Dimethoxy-3-hydroxyflavone (DMF-OH) (1-10 μM, 6-48 h) can inhibit high glucose-induced PAR4 expression in the endothelial cells of EA.hy 926 cells [1]. 7,4'-Dimethoxy-3-hydroxyflavone (1-10 μM, 6-48 h) can inhibit high glucose-induced endothelial PAR4 function by eliminating PAR4-mediated Ca2+ response and reducing the Ca2+ response of EA.hy 926 cells to AYPGKF-NH₂ (PAR4 activating peptide) or thrombin [1]. 7,4'-Dimethoxy-3-hydroxyflavone (1-10 μM, 24 h) can inhibit the PAR4-mediated exacerbation of high glucose-induced EA.hy 926 cell endothelial dysfunction [1]. 7,4'-Dimethoxy-3-hydroxyflavone (1-10 μM, 24 h) inhibited PAR4 expression in high glucose-induced EA.hy 926 cells by suppressing ROS-driven NF-κB activation [1]. 7,4'-Dimethoxy-3-hydroxyflavone (1-5 μM, 3-5 min) inhibited PAR4-mediated human platelet aggregation and secretion by suppressing GPIIb/IIIa activation, which is a key step in PAR4-AP-induced platelet aggregation [2]. 7,4'-Dimethoxy-3-hydroxyflavone (1-5 μM, 1-3 min) inhibited downstream signaling pathways of PAR4 in platelets, including Ca2+/protein kinase C, Akt, ERK, and p38 [2]. 7,4'-Dimethoxy-3-hydroxyflavone (5-20 μM, 10 min) inhibited the recruitment of β-arrestin to PAR4 in CHO-K1 cells in a concentration-dependent manner [2]. 7,4'-Dimethoxy-3-hydroxyflavone (5-20 μM, 3 min) enhanced the inhibitory effects of Vorapaxar and Ticagrelor on thrombin-induced platelet aggregation [2]. 7,4'-Dimethoxy-3-hydroxyflavone (5-10 μM, 10 min) reduced thrombus formation in whole blood under flowing conditions [2].
|
|---|---|
| ln Vivo |
7,4'-Dimethoxy-3-hydroxyflavone (DMF-OH) (20 mg/kg, gavage, once daily for 21 days) inhibited vascular PAR4 expression and endothelial dysfunction in streptozotocin (STZ)-induced diabetic mice and improved oxidative stress [1]. 7,4'-Dimethoxy-3-hydroxyflavone (1-7.5 mg/kg, intraperitoneal injection, single dose) significantly protected mice from FeCl3-induced carotid artery occlusion without significantly affecting tail bleeding time [2].
|
| Cell Assay |
Real-time quantitative PCR[1]
Cell Types: EA.hy926 cells in high glucose (HG) culture. Tested Concentrations: 1, 3, 10 μM Incubation Duration: 6 hours Experimental Results: High glucose-induced F2RL3 expression was inhibited in a concentration-dependent manner, and complete inhibition was achieved at 10 μM. Western Blot analysis [1] Cell Types: EA.hy926 cells were cultured under high glucose (HG) conditions. Tested Concentrations: 10 μM Culture time: 48 hours Experimental Results: High glucose-induced PAR4 protein expression was inhibited. Real-time quantitative PCR[1] Cell Types: EA.hy926 cells cultured in high glucose (HG) Tested Concentrations: 1, 10 μM Culture time: 24 hours Experimental Results: The expression of VCAM1, ICAM1, CCL2, TNF, IL1B and F3 was reduced.
|
| Animal Protocol |
Animal/Disease Models:Four-week-old male C57BL/6J mice were intraperitoneally injected with STZ (180 mg/kg) [1]
Doses: 20 mg/kg Route of Administration: Daily gavage for 21 days Experimental Results: No effect on STZ-induced hyperglycemia and weight loss. Inhibited upregulation of PAR4. Improved aortic wall thickening and disordered arrangement of tunica media smooth muscle cells. Inhibited the increase in expression of pro-inflammatory and procoagulant mediators in the aorta and prevented macrophage infiltration. Prevented the increase in aortic 8-OHdG levels induced by diabetes. Reduced serum MDA levels. Animal/Disease Models:Male Balb/c mice (20-25 g, 6-8 weeks old) FeCl3-induced arterial thrombosis model [2] Doses: 1, 3 and 7.5 mg/kg Route of Administration: Intraperitoneal injection 30 minutes before thrombosis induction Experimental Results: Prevented thrombosis in mice without affecting bleeding time |
| References |
|
| Molecular Formula |
C17H14O5
|
|---|---|
| Molecular Weight |
298.29
|
| CAS # |
13198-99-7
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
COC1=CC=C(C=C1)C2=C(C(C3=CC=C(C=C3O2)OC)=O)O
|
| 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) |
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
|
|---|---|
| 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 | 3.3524 mL | 16.7622 mL | 33.5244 mL | |
| 5 mM | 0.6705 mL | 3.3524 mL | 6.7049 mL | |
| 10 mM | 0.3352 mL | 1.6762 mL | 3.3524 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.