Terutroban
Based on 1 publication(s) in Google Scholar
Terutroban (S-18886) is a selective and orally active thromboxane-prostaglandin (TP) receptor antagonist with an IC50 of 16.4 nM. Terutroban inhibits TXA2 and prostaglandin endoperoxide receptors. Terutroban is a potent antithrombotic agent and possesses anti-atherosclerotic and anti-vasoconstrictor properties.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.84%
- CAS. Nr.: 165538-40-9
- Formel: C20H22ClNO4S
- Molecular Weight:407.91
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Publications Citing Use of MedChemExpress (MCE) Terutroban
More
Biologische Aktivität
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293-A | IC50 |
16.4 nM
Compound: 1, S-18886
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Antagonist activity against human thromboxane A2 receptor alpha expressed in QBI-HEK293A cells assessed as reduction in I-BOP-induced inositol monophosphate production incubated for 15 to 60 mins before I-BOP addition by HTRF assay
Antagonist activity against human thromboxane A2 receptor alpha expressed in QBI-HEK293A cells assessed as reduction in I-BOP-induced inositol monophosphate production incubated for 15 to 60 mins before I-BOP addition by HTRF assay
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[PMID: 25221659] |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male spontaneously hypertensive stroke-prone rats (SHRSPs) +Fed a high-sodium permissive diet and received 1% NaCl in drinking water[2]
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Dosage:30 mg/kg
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Administration:i.g., once a day, for 6 weeks
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Result:Significant reduced the aortic media thickness-to-lumen ratio.
Significantly decreased the number of bromodeoxyuridine-positive and proliferating cell nuclear antigen-positive cells in the media.
Completely prevented severe fibrosis in the vascular wall, characterized by the accumulation of collagen and fibronectin.
Chemical Information
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CAS. Nr. 165538-40-9
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Appearance Solid
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Molecular Weight 407.91
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Formel C20H22ClNO4S
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Color White to off-white
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SMILES
O=C(O)CCC1=C2CC[C@@H](NS(=O)(C3=CC=C(Cl)C=C3)=O)CC2=CC=C1C
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Synonyms
S-18886
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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Med Sci Monit
2020 Jun 18;26:e923163. PMID: 32555127
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (245.15 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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: ≥ 2.5 mg/mL (6.13 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Reinheit & Dokumentation
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Data Sheet (275 KB)
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SDS (393 KB)
- English - EN (393 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Wang X, et al. Potent, long-acting cyclopentane-1,3-Dione thromboxane (A2)-receptor antagonists. ACS Med Chem Lett. 2014 Jul 24;5(9):1015-20. [Content Brief]
[2]. Gelosa P, et al. Terutroban, a thromboxane/prostaglandin endoperoxide receptor antagonist, prevents hypertensive vascular hypertrophy and fibrosis. Am J Physiol Heart Circ Physiol. 2011 Mar;300(3):H762-8. [Content Brief]
[3]. Lesault PF, et al. Daily administration of the TP receptor antagonist terutroban improved endothelial function in high-cardiovascular-risk patients with atherosclerosis. Br J Clin Pharmacol.2011 Jun;71(6):844-851. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4515 mL | 12.2576 mL | 24.5152 mL | 61.2880 mL |
| 5 mM | 0.4903 mL | 2.4515 mL | 4.9030 mL | 12.2576 mL | |
| 10 mM | 0.2452 mL | 1.2258 mL | 2.4515 mL | 6.1288 mL | |
| 15 mM | 0.1634 mL | 0.8172 mL | 1.6343 mL | 4.0859 mL | |
| 20 mM | 0.1226 mL | 0.6129 mL | 1.2258 mL | 3.0644 mL | |
| 25 mM | 0.0981 mL | 0.4903 mL | 0.9806 mL | 2.4515 mL | |
| 30 mM | 0.0817 mL | 0.4086 mL | 0.8172 mL | 2.0429 mL | |
| 40 mM | 0.0613 mL | 0.3064 mL | 0.6129 mL | 1.5322 mL | |
| 50 mM | 0.0490 mL | 0.2452 mL | 0.4903 mL | 1.2258 mL | |
| 60 mM | 0.0409 mL | 0.2043 mL | 0.4086 mL | 1.0215 mL | |
| 80 mM | 0.0306 mL | 0.1532 mL | 0.3064 mL | 0.7661 mL | |
| 100 mM | 0.0245 mL | 0.1226 mL | 0.2452 mL | 0.6129 mL |
Terutroban Related Classifications
HY-16991 Related Classifications
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