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Ethamsylate (E-141; MD-141; Aglumin; Altodor; Eselin), a benzenesulfonate analogue, is an antihemorrhagic drug (haemostatic drug) which works by increasing resistance in the endothelium of capillaries and promoting platelet adhesion. Moreover, it suppresses the production and function of prostaglandins that lead to vasodilation, enhanced capillary permeability, and platelet disaggregation.
| Targets |
prostaglandins
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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]
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| 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]
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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. |
| Animal Protocol |
C57BL/6J female mice of spinal cord injury
100 mg/kg Oral gavage (p.o.), twice a day, three days |
| References |
| Molecular Formula |
C10H17NO5S
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|---|---|
| Molecular Weight |
263.308
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| Exact Mass |
263.08
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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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| Appearance |
Solid powder
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| SMILES |
CCNCC.C1=CC(=C(C=C1O)S(=O)(=O)O)O
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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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