| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
5-LO 5 μM (IC50) COX-1 0.65 μg/mL (IC50) COX-2 1.2 μg/mL (IC50)
BW755C targets the cyclooxygenase (COX) and 5-lipoxygenase (5-LO) enzymes. It is a potent dual inhibitor. For the LOX pathway, it inhibits 5-LO with an IC50 of 5 microM. For the COX pathway, it inhibits COX-1 and COX-2 with IC50 values of 0.65 microg/mL and 1.2 microg/mL, respectively. By simultaneously blocking the production of prostaglandins and leukotrienes, it exerts a broad anti-inflammatory effect. |
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| ln Vitro |
In vitro, BW755C is a dual inhibitor of the COX and 5-LO pathways. It inhibits 5-lipoxygenase (5-LO) with an IC50 of 5 microM. It also inhibits cyclooxygenase (COX), with IC50s of 0.65 microg/mL for COX-1 and 1.2 microg/mL for COX-2. This combined inhibition of both major branches of the arachidonic acid cascade makes it a powerful tool for studying the role of eicosanoids in cellular models of inflammation and cancer.
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| ln Vivo |
Rats' ovarian 5-HETE and 12-HETE levels as well as their ovulation rate are inhibited by BW 755C (0.03-10 mg/rat; sc; once)[3].
In vivo, BW755C has been shown to delay neuronal death in an animal model of ischemia. In a study on Mongolian gerbils, administration of BW755C (30 mg/kg) following 5 minutes of forebrain ischemia resulted in a neuronal density of 14 in the hippocampal CA1 sector 7 days post-insult, compared to a density of 13 in vehicle-treated ischemic animals. This demonstrates that BW755C can provide neuroprotection, an effect attributed to its anti-inflammatory properties. |
| Enzyme Assay |
Cell-free enzyme assays are used to confirm the dual inhibitory activity of BW755C. For 5-LO inhibition, the enzyme is incubated with BW755C (e.g., 0.1-100 uM) and arachidonic acid. For COX inhibition, ovine COX-1 or human recombinant COX-2 is used. The reaction products are quantified to calculate the specific IC50 values. The published values are 5 uM for 5-LO, 0.65 microg/mL for COX-1, and 1.2 microg/mL for COX-2.
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| Cell Assay |
For cellular assays, human whole blood or isolated PBMCs are pre-incubated with BW755C. For assessing COX-1/2 activity, blood is incubated with the compound, and the blood is allowed to clot; serum thromboxane B2 (a COX-1 product) is measured by ELISA. For COX-2 activity, LPS-stimulated blood is used to measure PGE2 production. For 5-LO activity, blood is incubated with the compound and then stimulated with calcium ionophore A23187 and LPS to generate LTB4. All products are quantified by ELISA.
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| Animal Protocol |
Animal/Disease Models: Immature Wistar rats ~22 days of age[3]
Doses: 0.03, 0.1, 0.3, 1.0, 3.1 and 10 mg/rat Route of Administration: subcutaneous (sc) injection, once Experimental Results: decreased 5-HETE (moderately) and 12-HETE ( strongly). In vivo neuroprotection studies with BW755C use a transient forebrain ischemia model in Mongolian gerbils. Animals are anesthetized, and both common carotid arteries are occluded for 5 minutes. BW755C (30 mg/kg) or vehicle is administered via intraperitoneal injection immediately after reperfusion. Seven days later, animals are perfusion-fixed, and their brains are sectioned. The neuronal density in the hippocampal CA1 sector is estimated histologically to assess the protective effect of the compound. |
| ADME/Pharmacokinetics |
Published pharmacokinetic data for BW755C is limited. The compound has a molecular weight of 229.3 g/mol. For in vivo use, it is administered intraperitoneally or orally. A common formulation is in sterile saline with a small percentage of DMSO. It is likely to have good oral absorption given its molecular properties, but formal PK studies would be required to determine parameters such as half-life, Cmax, and oral bioavailability in any animal model.
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| Toxicity/Toxicokinetics |
Publicly available toxicology data for BW755C is not detailed. In cell-based assays at concentrations used for enzyme inhibition (up to 10-20 uM), no overt toxicity is typically reported. In animal studies, a dose of 30 mg/kg administered intraperitoneally was reported to be well-tolerated without significant adverse effects in the gerbil ischemia model. Standard safety precautions for handling research chemicals should be followed.
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| References |
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| Additional Infomation |
It is a dual inhibitor of the cyclooxygenase and lipoxygenase pathways. It exerts its anti-inflammatory effect by inhibiting the production of prostaglandins and leukotrienes. This drug also enhances pulmonary hypoxic vasoconstriction and has a protective effect after myocardial ischemia.
BW755C is a research-grade compound and has not been approved for clinical use. As a classic dual COX/5-LO inhibitor, it has played a foundational role in pharmacological research, helping to dissect the complex roles of eicosanoids in inflammation, pain, and cardiovascular diseases. The compound should be stored at -20degC as a powder, protected from light and moisture. For research use only. |
| Molecular Formula |
C10H10F3N3
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|---|---|
| Molecular Weight |
229.20
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| Exact Mass |
229.082
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| CAS # |
66000-40-6
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| PubChem CID |
47795
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| Appearance |
Brown to reddish brown solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
308.5±52.0 °C at 760 mmHg
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| Flash Point |
140.4±30.7 °C
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| Vapour Pressure |
0.0±0.7 mmHg at 25°C
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| Index of Refraction |
1.559
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| LogP |
1.94
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
16
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| Complexity |
288
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1CN(N=C1N)C2=CC=CC(=C2)C(F)(F)F
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| InChi Key |
CPXGGWXJNQSFEP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C10H10F3N3/c11-10(12,13)7-2-1-3-8(6-7)16-5-4-9(14)15-16/h1-3,6H,4-5H2,(H2,14,15)
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| Chemical Name |
2-[3-(trifluoromethyl)phenyl]-3,4-dihydropyrazol-5-amine
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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) |
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
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| 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 | 4.3630 mL | 21.8150 mL | 43.6300 mL | |
| 5 mM | 0.8726 mL | 4.3630 mL | 8.7260 mL | |
| 10 mM | 0.4363 mL | 2.1815 mL | 4.3630 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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