| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
Thromboxane synthase (TXA2 synthase).
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|---|---|
| ln Vitro |
Dazoxiben selectively inhibits thromboxane synthase, blocking the synthesis of thromboxane A2 (TXA2). TXA2 is a potent vasoconstrictor and platelet aggregator. By inhibiting its production, Dazoxiben reduces vasoconstriction and platelet aggregation, leading to antithrombotic effects.
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| ln Vivo |
In vivo, Dazoxiben is orally active and has been shown to inhibit platelet function and improve blood flow. It has demonstrated significant clinical improvement in patients with Raynaud's syndrome. It has been studied for its potential in treating cardiovascular diseases and thrombotic disorders.
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| Enzyme Assay |
Dazoxiben is evaluated in cell-free enzyme assays using purified thromboxane synthase. The compound is incubated with the enzyme and a substrate (e.g., prostaglandin H2), and the inhibition of TXA2 production is measured. IC50 values are determined to quantify the potency of thromboxane synthase inhibition.
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| Cell Assay |
Dazoxiben is assessed in cell-based assays using platelets or other relevant cell types. Platelet aggregation assays are performed to evaluate the functional effects of thromboxane synthase inhibition. Platelets are treated with Dazoxiben and stimulated with agonists, and aggregation is measured using aggregometry.
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| Animal Protocol |
Dazoxiben is administered orally in animal models to evaluate its antithrombotic and cardiovascular effects. Efficacy is assessed in models of thrombosis, where parameters such as platelet aggregation, thrombus formation, and blood flow are measured. It has also been studied in models of Raynaud's syndrome.
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| ADME/Pharmacokinetics |
Dazoxiben is orally active. No detailed PK parameters (T1/2, Cmax, AUC) are available. Molecular formula: C12H12N2O3; MW: 232.24.
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| Toxicity/Toxicokinetics |
No detailed toxicity data available. For research use only. As a thromboxane synthase inhibitor, potential side effects would include bleeding risk.
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| References | |
| Additional Infomation |
Dazoxiben (UK-37248) is an orally active thromboxane synthase inhibitor. Molecular formula: C12H12N2O3; MW: 232.24. Investigated for Raynaud's syndrome. For research use only.
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| Molecular Formula |
C30H36BR2N4O2
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|---|---|
| Molecular Weight |
644.452
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| Exact Mass |
232.085
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| CAS # |
78218-09-4
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| Related CAS # |
74226-22-5 (HCl);78218-09-4;
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| PubChem CID |
53001
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.25 g/cm3
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| Boiling Point |
491.2ºC at 760 mmHg
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| Melting Point |
230-235°C
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| Flash Point |
250.9ºC
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| Index of Refraction |
1.593
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| LogP |
1.66
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
17
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| Complexity |
252
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| Defined Atom Stereocenter Count |
0
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| SMILES |
0
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| InChi Key |
PVKDFUXBDJPRGU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C12H12N2O3.ClH/c15-12(16)10-1-3-11(4-2-10)17-8-7-14-6-5-13-9-14/h1-6,9H,7-8H2,(H,15,16)1H
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| Chemical Name |
4-(2-(1H-Imidazol-1-yl)ethoxy)benzoic acid hydrochloride
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| Synonyms |
UK-37248 UK37248 UK-37,248-01.
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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 | 1.5517 mL | 7.7586 mL | 15.5171 mL | |
| 5 mM | 0.3103 mL | 1.5517 mL | 3.1034 mL | |
| 10 mM | 0.1552 mL | 0.7759 mL | 1.5517 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.
Products are for research use only; We do not sell to patients
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