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| 1mg |
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| 5mg |
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| Targets |
Thromboxane A2 (TXA2) receptor. Daltroban is a selective and specific thromboxane A2 receptor antagonist. By blocking TXA2 receptors, it inhibits platelet aggregation and vasoconstriction. The compound helps prevent thrombosis and improve blood flow. It also exhibits anti-inflammatory effects by modulating prostanoid pathways.
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| ln Vitro |
Daltroban is a selective and specific thromboxane A2 receptor antagonist. It inhibits platelet aggregation and vasoconstriction. The compound increases intracellular calcium in vascular smooth muscle cells. It exerts protective effects on brain infarction in vitro and heart cell injury due to hypoxia and hypoglycemia. It lowers serum CPK activity in vitro.
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| ln Vivo |
In cats suffering from acute myocardial ischemia, daltroban (BM-13505) (1 mg/kg; intravenously; hourly) protects against reperfusion injury [2]. Compared to cats given with vehicle (saline), datroban (20 mg/kg/hour, intravenously) decreased ischemia-induced ST-segment elevation and avoided the development of Q waves on the ECG following reperfusion. Datroban prevents leukocytosis brought on by ischemia, which shields the heart from ischemic damage [3].
Daltroban protects the myocardium from ischemic injury and suppresses leukocytosis. It helps prevent thrombosis and improve blood flow, particularly in conditions like myocardial infarction and stroke. The compound exerts protective effects on brain infarction. It exhibits anti-inflammatory effects by modulating prostanoid pathways. |
| Enzyme Assay |
Daltroban is evaluated in cell-free receptor binding assays using membrane preparations expressing TXA2 receptors. Radioligand binding displacement assays are performed to determine the affinity of Daltroban for the TXA2 receptor. Competition binding experiments are conducted with increasing concentrations of Daltroban and a fixed concentration of a labeled reference ligand.
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| Cell Assay |
Daltroban is assessed in cell-based assays using vascular smooth muscle cells and platelets. The compound's ability to inhibit platelet aggregation is measured using aggregometry. Its effects on intracellular calcium levels in vascular smooth muscle cells are assessed. Protective effects on heart cell injury due to hypoxia and hypoglycemia are evaluated.
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| Animal Protocol |
Animal/Disease Models: Adult male cat (2.8 to 4.6 kg; anesthetized cat model) [2]
Doses: 1 mg/kg Route of Administration: IV; 1 mg/kg 30 minutes before reperfusion, then 1 mg/kg kg/hour Experimental Results: Significant reduction of ischemic tissue area as a percentage of total left ventricular mass and total area at risk without altering basic hemodynamics and therefore without affecting myocardial oxygen demand. Daltroban is administered in animal models to evaluate its protective effects on myocardial ischemia and brain infarction. It protects the myocardium from ischemic injury and suppresses leukocytosis. The compound helps prevent thrombosis and improve blood flow. It exhibits anti-inflammatory effects. |
| ADME/Pharmacokinetics |
Daltroban has a molecular weight of 353.82 and a molecular formula of C16H16ClNO4S. It has a CAS number of 79094-20-5. The compound is soluble in DMSO at 22 mg/mL. It should be stored as a powder at -20°C for up to 3 years. It is a selective TXA2 receptor antagonist.
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| Toxicity/Toxicokinetics |
No detailed toxicity data is available for Daltroban. The compound is for research use only and is not intended for human therapeutic use. It has been studied for its potential in treating cardiovascular diseases. Specific toxicity studies have not been well-characterized.
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| References |
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| Additional Infomation |
Daltroban (BM-13505) is a selective and specific thromboxane A2 (TXA2) receptor antagonist. It has a molecular weight of 353.82 and a molecular formula of C16H16ClNO4S. The compound has a CAS number of 79094-20-5. It inhibits platelet aggregation and vasoconstriction. It protects the myocardium from ischemic injury and suppresses leukocytosis. The compound is for research use only and has not been approved for clinical use.
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| Molecular Formula |
C16H16NO4SCL
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|---|---|
| Molecular Weight |
353.82054
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| Exact Mass |
353.049
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| CAS # |
79094-20-5
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| PubChem CID |
54343
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| Appearance |
White to light yellow solid powder
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| Density |
1.378g/cm3
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| Boiling Point |
555.3ºC at 760 mmHg
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| Melting Point |
132.5-137.4 °C(lit.)
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| Flash Point |
289.6ºC
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| Vapour Pressure |
3.63E-13mmHg at 25°C
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| Index of Refraction |
1.609
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| LogP |
3.959
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
23
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| Complexity |
475
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
IULOBWFWYDMECP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H16ClNO4S/c17-14-5-7-15(8-6-14)23(21,22)18-10-9-12-1-3-13(4-2-12)11-16(19)20/h1-8,18H,9-11H2,(H,19,20)
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| Chemical Name |
2-[4-[2-[(4-chlorophenyl)sulfonylamino]ethyl]phenyl]acetic acid
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 | 2.8263 mL | 14.1315 mL | 28.2630 mL | |
| 5 mM | 0.5653 mL | 2.8263 mL | 5.6526 mL | |
| 10 mM | 0.2826 mL | 1.4131 mL | 2.8263 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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