Ethamsylate
Based on 1 Customer Validation
Ethamsylate (Etamsylate) is an orally active anti-hemorrhagic compound. Ethamsylate inhibits biosynthesis and action of prostaglandins. Ethamsylate has the potential to maintain early hemostasis as well as restores capillary resistance. Ethamsylate acts as an antiangiogenic factor, inhibiting wound healing and matrigel tubulogenesis..
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- Reinheit: 99.49%
- CAS. Nr.: 2624-44-4
- Formel: C10H17NO5S
- Molecular Weight:263.31
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Speicherung:
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
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Biologische Aktivität
Ethamsylate (480 μM, 30 mim) prolongs lifetime of neutrophils[1].
Ethamsylate (0-100 μM, 3-8 h) inhibits migration and tubulogenesis on matrigel in endothelial cells[3].
Ethamsylate (0-100 μM, 48 h), inhibits the signaling of FGF/FGFR, decreases phosphorylation Levels of AKT and Erk1/2[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HMEC-1 and HUVECs cells
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Concentration:0-100 μM
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Incubation Time:3-8 h
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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.
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Cell Line:HUVECs cells
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Concentration:0-100 μM
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Incubation Time:48 h
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Result:Decreased the amount of Akt1 phosphorylated.
Decreased pERK2 levels at the highest doses (50-100 μM).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J female mice of spinal cord injury[3]
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Dosage:100 mg/kg
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Administration:Oral gavage (p.o.), twice a day, three days
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Result:Attenuated the MMP-9 expression.
Inhibited the degradation of TJ proteins.
Reduced the upregulation of IL-1β, IL-6, and TNF-α.
Reduced axonal demyelination and decreased cystic cavity formation.
Reduced the extent of Fibrotic scar formation.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 2624-44-4
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Appearance Solid
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Molecular Weight 263.31
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Formel C10H17NO5S
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Color White to off-white
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SMILES
O=S(C1=CC(O)=CC=C1O)(O)=O.CCNCC
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Synonyms
Etamsylate
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Lösungsmittel & Löslichkeit
DMSO : 120 mg/mL (455.74 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 50 mg/mL (189.89 mM; Need ultrasonic)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 3 mg/mL (11.39 mM); Clear solution
This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 3 mg/mL (11.39 mM); Clear solution
This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 100 mg/mL (379.78 mM); Clear solution; Need ultrasonic
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Reinheit & Dokumentation
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Data Sheet (283 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Zawrotniak M, et al. Selected mucolytic, anti-inflammatory and cardiovascular drugs change the ability of neutrophils to form extracellular traps (NETs). Acta Biochim Pol. 2015;62(3):465-73. [Content Brief]
[2]. Kovács L, et al. Etamsylate as inhibitor of prostaglandin biosynthesis in pregnant human myometrium in vitro. Experientia. 1981 Nov 15;37(11):1182-3. [Content Brief]
[3]. Albiñana V, et al. Topically Applied Etamsylate: A New Orphan Drug for HHT-Derived Epistaxis (Antiangiogenesis through FGF Pathway Inhibition). TH Open. 2019 Jul 26;3(3):e230-e243. [Content Brief]
[4]. Dolma S, et al. Ethamsylate Attenuates Mutilated Secondary Pathogenesis and Exhibits a Neuroprotective Role in Experimental Model of Spinal Cord Injury. Neuroscience. 2022 Feb 21;484:26-37. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| H2O / DMSO | 1 mM | 3.7978 mL | 18.9890 mL | 37.9780 mL | 94.9451 mL |
| 5 mM | 0.7596 mL | 3.7978 mL | 7.5956 mL | 18.9890 mL | |
| 10 mM | 0.3798 mL | 1.8989 mL | 3.7978 mL | 9.4945 mL | |
| 15 mM | 0.2532 mL | 1.2659 mL | 2.5319 mL | 6.3297 mL | |
| 20 mM | 0.1899 mL | 0.9495 mL | 1.8989 mL | 4.7473 mL | |
| 25 mM | 0.1519 mL | 0.7596 mL | 1.5191 mL | 3.7978 mL | |
| 30 mM | 0.1266 mL | 0.6330 mL | 1.2659 mL | 3.1648 mL | |
| 40 mM | 0.0949 mL | 0.4747 mL | 0.9495 mL | 2.3736 mL | |
| 50 mM | 0.0760 mL | 0.3798 mL | 0.7596 mL | 1.8989 mL | |
| 60 mM | 0.0633 mL | 0.3165 mL | 0.6330 mL | 1.5824 mL | |
| 80 mM | 0.0475 mL | 0.2374 mL | 0.4747 mL | 1.1868 mL | |
| 100 mM | 0.0380 mL | 0.1899 mL | 0.3798 mL | 0.9495 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Ethamsylate Related Classifications
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