| Size | Price | Stock | Qty |
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| 500mg |
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| 1g |
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| 2g |
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| 10g | |||
| Other Sizes |
| Targets |
prostaglandins
Ethamsylate's precise mechanism of action is not fully understood, but it is thought to act by multiple mechanisms. It improves platelet adhesiveness and promotes P-selectin-dependent, platelet adhesive mechanisms. It also restores capillary resistance and inhibits prostaglandin biosynthesis, which reduces platelet disaggregation and capillary permeability. |
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| ln Vitro |
Ethamsylate has an IC50 of 0.5 mM and inhibits prostaglandin biosynthesis in microsomes of human pregnant myometrium.[1] Ethamsylate is particularly active against hydroxyl radicals (OH.), which are scavenged at therapeutic Ethamsylate concentrations (0.1–10 μM). To scavenge superoxide radicals, higher concentrations of ethhamsylate are needed. The effects of arachidonic acid, thromboxane A2, collagen, and calcium ionophore A23187 on human platelet aggregation and ATP release are enhanced by ethamsylate.[2]
In vitro studies have shown that ethamsylate promotes platelet/leukocyte aggregate formation. It introduces platelets into a priming state and enhances their procoagulant response. However, reproducing ethamsylate's in vitro results can be challenging, and its mechanism of action is still being investigated. |
| ln Vivo |
Ethamsylate lowers the mean bleeding time when given systemically or orally to rabbits. Ethamsylate, when administered intravenously, reduces bleeding time in half at doses greater than 5 mg/kg. The effect begins to take effect five minutes after the injection, peaks between thirty minutes and four hours later, and then fades away six hours later. A comparable maximal effect is seen when taking the medication orally, with a dosage of 10 mg/kg. Ethamsylate's ability to lessen intraventricular hemorrhage is linked to a decrease in the production of prostacyclin and thromboxane A2. Ethamsylate (>25 mg/kg) administered orally also prevents rat paw edema caused by carrageenan. [2]
Ethamsylate is used in vivo as a hemostatic agent to control bleeding in various clinical settings. It is indicated in cases of capillary bleeding and is used to reduce blood loss during surgery and in conditions such as menorrhagia. Its efficacy is based on its ability to improve platelet function and capillary integrity. |
| Enzyme Assay |
Non-cellular assays for ethamsylate are limited, as its activity is primarily assessed in whole blood or platelet-rich plasma. Its effects on platelet function can be studied using aggregometry, where platelet aggregation is induced by agonists in the presence of ethamsylate. Its inhibition of prostaglandin biosynthesis can be assessed using enzyme assays with arachidonic acid as a substrate.
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| Cell Assay |
Cell Line: HMEC-1 and HUVECs cells
Concentration: 0-100 μM Incubation Time: 3-8 h Result: Didn’t affect the migration of HMEC-1 cells. Inhibited the migration of HUVECs cells. Thinned the morphology of the closed network and enlarged the closed cells. In vitro cellular assays for ethamsylate involve treating platelet-rich plasma or whole blood with the compound and measuring platelet function. Platelet adhesiveness is assessed using standard adhesion assays. Platelet aggregation is measured using light transmission aggregometry or impedance aggregometry in response to various agonists. The formation of platelet/leukocyte aggregates is assessed by flow cytometry. |
| Animal Protocol |
C57BL/6J female mice of spinal cord injury
100 mg/kg Oral gavage (p.o.), twice a day, three days In vivo animal experiments with ethamsylate are conducted in models of bleeding. Rodents are subjected to a standardized injury (e.g., tail transection, liver laceration) and treated with ethamsylate via intravenous or oral administration. The volume of blood loss and the time to hemostasis are measured. The compound's effects on platelet function and capillary resistance are assessed ex vivo. |
| ADME/Pharmacokinetics |
Ethamsylate has a molecular weight of 263.31 and a molecular formula of C₁₀H₁₇NO₅S. It is a white crystalline powder with a purity of ≥98%. The compound is soluble in water and is typically stored at room temperature in a dry place. Following intravenous or oral administration, it is rapidly distributed and eliminated, primarily via the kidneys.
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| Toxicity/Toxicokinetics |
Ethamsylate is generally well-tolerated at therapeutic doses. Side effects are rare but may include gastrointestinal disturbances, headache, and allergic reactions. It is contraindicated in patients with known hypersensitivity to the drug. Standard safety precautions should be followed when handling the compound.
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| References | |
| Additional Infomation |
Etamsylate sulfonate is a sulfonic acid derivative and an organosulfur compound. Benzenesulfonate derivatives are used as systemic hemostatic agents. See also: Dobexic acid (containing the active portion).
Ethamsylate (CAS 2624-44-4) is a synthetic hemostatic agent that improves platelet adhesiveness and restores capillary resistance. It promotes P-selectin-dependent platelet adhesive mechanisms and inhibits prostaglandin biosynthesis. It is used to treat capillary bleeding and is available as an injectable and oral formulation. Ethamsylate remains a valuable tool in hemostasis research. |
| Molecular Formula |
C10H17NO5S
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|---|---|
| Molecular Weight |
263.308
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| Exact Mass |
263.082
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| Elemental Analysis |
C, 45.62; H, 6.51; N, 5.32; O, 30.38; S, 12.18
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| CAS # |
2624-44-4
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| PubChem CID |
17506
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| Appearance |
White to off-white solid powder
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| Boiling Point |
496.4ºC at 760 mmHg
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| Melting Point |
127-131ºC
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| Flash Point |
254ºC
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| Vapour Pressure |
1.13E-10mmHg at 25°C
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| LogP |
2.432
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
3
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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 |
S(C1C([H])=C(C([H])=C([H])C=1O[H])O[H])(=O)(=O)O[H].N([H])(C([H])([H])C([H])([H])[H])C([H])([H])C([H])([H])[H]
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| InChi Key |
HBGOLJKPSFNJSD-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C6H6O5S.C4H11N/c7-4-1-2-5(8)6(3-4)12(9,10)11;1-3-5-4-2/h1-3,7-8H,(H,9,10,11);5H,3-4H2,1-2H3
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| Chemical Name |
2,5-dihydroxybenzenesulfonic acid;N-ethylethanamine
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| Synonyms |
MD 141; E 141; E141; MD141; Ethamsylate; E 141; MD 141; E-141; MD-141; Aglumin; Altodor; Eselin
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| HS Tariff Code |
2934.99.03.00
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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: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), 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) |
DMSO: 53~120 mg/mL (201.3~455.7 mM)
Water: ~53 mg/mL |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 3 mg/mL (11.39 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 30.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 3 mg/mL (11.39 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 30.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 3 mg/mL (11.39 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 100 mg/mL (379.78 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.7978 mL | 18.9890 mL | 37.9780 mL | |
| 5 mM | 0.7596 mL | 3.7978 mL | 7.5956 mL | |
| 10 mM | 0.3798 mL | 1.8989 mL | 3.7978 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT06190535 | Not yet recruiting | Drug: Etamsylate | Postpancreatectomy Hemorrhage | University of Sfax | January 1, 2024 | Not Applicable |
| NCT04656067 | Completed | Drug: Oxytocin ,Tranexamic acid and Ethamsylate |
Blood Loss, Surgical Blood Loss, Postoperative |
Egymedicalpedia | April 1, 2020 | Phase 1 Phase 2 |
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