BW 755C |
| Catalog No.GC14601 |
dual inhibitor of 5-lipoxygenase (5-LO) and cyclooxygenase (COX) pathways
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 66000-40-6
Sample solution is provided at 25 µL, 10mM.
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IC50: 0.75 μM, 0.65 μg/ml, and 1.2 μg/ml for 5-LO, COX-1, and COX-2, respectively
BW 755C is a dual inhibitor of 5-lipoxygenase (5-LO) and cyclooxygenase (COX) pathways.
Constitutive cyclooxygenase (COX-1) is present in cells under physiological conditions, whereas COX-2 is induced by some cytokines, mitogens, and endotoxin in pathological conditions, such as inflammation. Since 5-lipoxygenase (5-LO) oxidizes arachidonic acid to 5-hydroperoxyeicosatetraenoic acid in the first step of the leukotriene pathway, 5-LO inhibitors should prevent leukotriene biosynthesis and thus prove useful in the treatment of allergic asthma.
In vitro: Previous study found that BW 755C and other nonsteroidal antiinflammatory drugs including diclofenac, acetaminophen, and naproxen showed approximately equipotent inhibitory effects on COX-1 and COX-2 in intact cells. Whereas, BF 389 was the most potent and most selective inhibitor of COX-2 in intact cells [1].
In vivo: An animal study was conducted to examine whether BW-755C delayed neuronal death in the hippocampal CA1 sector in Mongolian gerbils after 5 minutes of forebrain ischemia. Gerbils were injected with BW-755C. Seven days after ischemic insult, the animals were perfusion-fixed, and the neuronal density in the hippocampal CA, sector was estimated. Results showed that in ischemic gerbils with vehicle administration, the average neuronal density was 13 for BW-755C. In ischemic gerbils treated with 30 mg/kg BW-755C, the average neuronal densities was 14 [2].
Clinical trial: So far, no clinical study has been conducted.
References:
[1] Mitchell, J. A.,Akarasereenont, P.,Thiemermann, C., et al. Selectivity of nonsteroidal antiinflammatory drugs as inhibitors of constitutive and inducible cyclooxygenase. Proceedings of the National Academy of Sciences of the United States of America 90, 11693-11697 (1993).
[2] Nakagomi T, Sasaki T, Kirino T, Tamura A, Noguchi M, Saito I, Takakura K. Effect of cyclooxygenase and lipoxygenase inhibitors on delayed neuronal death in the gerbil hippocampus. Stroke. 1989 Jul;20(7):925-9.
| Cas No. | 66000-40-6 | SDF | |
| Chemical Name | 4,5-dihydro-1-[3-(trifluoromethyl)phenyl]-1H-pyrazol-3-amine | ||
| Canonical SMILES | NC(CC1)=NN1C2=CC=CC(C(F)(F)F)=C2 | ||
| Formula | C10H10F3N3 | M.Wt | 229.3 |
| Solubility | ≤30mg/ml in ethanol;30mg/ml in DMSO;25mg/ml in dimethyl formamide | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 4.3611 mL | 21.8055 mL | 43.611 mL |
| 5 mM | 0.8722 mL | 4.3611 mL | 8.7222 mL |
| 10 mM | 0.4361 mL | 2.1805 mL | 4.3611 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 19 reference(s) in Google Scholar.)
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