Ozagrel
Based on 1 publication(s) in Google Scholar
Ozagrel (OKY-046) is a high selective and orally active thromboxane A2 (TXA2) synthase inhibitor with an IC50 of 11 nM. Ozagrel exerts anti-platelet aggregation, vasodilation and anti-inflammatory effects by inhibiting the production of TXA2 and increasing the production of prostacyclin (PGI2). Ozagrel can be used for the study of ischemic stroke, asthma and thromboembolic diseases.
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- Pureza: 99.81%
- No. CAS: 82571-53-7
- Fòrmula: C13H12N2O2
- Peso molecular:228.25
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) Ozagrel
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Actividad biológica
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TXA2/TP 11 nM () |
TXB2 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Platelet | IC50 |
0.36 mM
Compound: Ozagrel
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Antiplatelet activity in rabbit platelet rich plasma assessed as inhibition of ADP-induced platelet aggregation after 5 mins by aggregometry
Antiplatelet activity in rabbit platelet rich plasma assessed as inhibition of ADP-induced platelet aggregation after 5 mins by aggregometry
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[PMID: 21993151] |
| Platelet | IC50 |
0.36 mM
Compound: Ozagrel
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Antiplatelet activity in rabbit platelet rich plasma assessed as inhibition of ADP-induced aggregation treated for 5 mins prior to ADP-challenge
Antiplatelet activity in rabbit platelet rich plasma assessed as inhibition of ADP-induced aggregation treated for 5 mins prior to ADP-challenge
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10.1039/C3MD20352B |
| Platelet | IC50 |
144.1 μM
Compound: Ozagrel
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Anti-platelet activity in rabbit platelet-rich plasma assessed as inhibition of ADP-induced platelet aggregation incubated for 5 mins at 37 degC by aggregometry
Anti-platelet activity in rabbit platelet-rich plasma assessed as inhibition of ADP-induced platelet aggregation incubated for 5 mins at 37 degC by aggregometry
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10.1039/C4MD00022F |
| Platelet | IC50 |
2.85 mM
Compound: Ozagrel
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Antiplatelet aggregation activity in rabbit platelet assessed as reduction in ADP-induced platelet aggregation
Antiplatelet aggregation activity in rabbit platelet assessed as reduction in ADP-induced platelet aggregation
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[PMID: 34902735] |
| Platelet | IC50 |
53.1 μM
Compound: Ozagrel
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Antiplatelet activity in human platelet rich plasma assessed as inhibition of arachidonic acid-induced platelet aggregation preincubated for 2 mins followed by arachidonic acid addition by turbidimetric method relative to control
Antiplatelet activity in human platelet rich plasma assessed as inhibition of arachidonic acid-induced platelet aggregation preincubated for 2 mins followed by arachidonic acid addition by turbidimetric method relative to control
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[PMID: 28453995] |
Ozagrel significantly inhibits platelet aggregation induced by Arachidonic acid (HY-109590) with an IC50 of 53.12 μM[1].
Ozagrel (100 μM) exhibits the inhibitory rate on plasma TXB2 of 99.6% but has no inhibitory effect on PGH2[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Ozagrel (80 mg/kg, i.v., single dose) attenuates lung injury and decreases monocyte chemoattractant protein-1 and interleukin-8 mRNA expression in Oleic acid (OA) (HY-N1446)-induced lung injury in guinea pigs[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:VI-L-Methionine-induced vascular cognitive impairment and dementia (VCID) model established in Wistar rats of both sex and weighing 200 g[2]
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Dosage:10 and 20 mg/kg
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Administration:Oral administration (p.o.), once daily for 21 days
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Result:Improved the endothelial dysfunction caused by L-methionine-induced impairment.
Shortened the latency period of evasion, increased the duration of stay in target quadrants and reduced the length of swimming path.
Significantly reduced cerebral TBARS levels, increased cerebral GSH content, inhibited cerebral AChE activity, and decreased cerebral MPO activity and levels of TNF-α and IL-6.
Reduced leukocyte infiltration, neuronal degeneration and necrosis, increased pyramidal neuron density.
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Animal Model:BCCAo induced vascular dementia (VaD) model established in Wistar rats of both sex and weighing 200 g[3]
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Dosage:10 and 20 mg/kg
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Administration:Oral administration (p.o.), once daily for 6 days
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Result:Improved the endothelial dysfunction caused by L-methionine-induced impairment.
Shortened the latency period of evasion, increased the duration of stay in target quadrants and reduced the length of swimming path.
Significantly reduced cerebral TBARS levels, increased cerebral GSH content, inhibited cerebral AChE activity, and decreased cerebral MPO activity and levels of TNF-α and IL-6.
Reduced neutrophil infiltration, alleviated neuronal degeneration and nuclear pyknosis, and improved vascular congestion state.
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Animal Model:OA-induced lung Injury model established in male Hartley guinea pigs (420-500 g) [4]
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Dosage:80 mg/kg
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Administration:Intravenous injection (i.v.), single dose, 3 h after OA injection
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Result:Significantly reduced the levels of TXB2 in BALF and plasma.
Reduced the expression of MCP-1 and IL-8 mRNA and the infiltration of macrophages and neutrophils.
Significantly reduced the total protein concentration in BALF.
Chemical Information
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No. CAS 82571-53-7
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Appearance Solid
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Peso molecular 228.25
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Fòrmula C13H12N2O2
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Color White to off-white
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SMILES
O=C(O)/C=C/C1=CC=C(CN2C=CN=C2)C=C1
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Synonyms
OKY-046
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
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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Nat Commun
Selective inhibition of cancer cell self-renewal through a Quisinostat-histone H1.0 axis. [Abstract]2020 Apr 14;11(1):1792. PMID: 32286289
Solvente y solubilidad
DMSO : 50 mg/mL (219.06 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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 (10.95 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (10.95 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 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.
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.
Pureza y Documentación
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Ficha de datos (278 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Saito MS, et al. Antiplatelet pyrazolopyridines derivatives: pharmacological, biochemical and toxicological characterization. J Enzyme Inhib Med Chem. 2016 Dec;31(6):1591-601. [Content Brief]
[2]. Bhatia P, Singh N. Ameliorative effect of ozagrel, a thromboxane A2 synthase inhibitor, in hyperhomocysteinemia-induced experimental vascular cognitive impairment and dementia. Fundam Clin Pharmacol. 2021 Aug;35(4):650-666. [Content Brief]
[3]. Bhatia P, Kaur G, Singh N. Ozagrel a thromboxane A2 synthase inhibitor extenuates endothelial dysfunction, oxidative stress and neuroinflammation in rat model of bilateral common carotid artery occlusion induced vascular dementia. Vascul Pharmacol. 2021 Apr;137:106827. [Content Brief]
[4]. Ishitsuka Y, et al. A selective thromboxane A2 (TXA2) synthase inhibitor, ozagrel, attenuates lung injury and decreases monocyte chemoattractant protein-1 and interleukin-8 mRNA expression in oleic acid-induced lung injury in guinea pigs. J Pharmacol Sci. 2009 Oct;111(2):211-5. [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 | 4.3812 mL | 21.9058 mL | 43.8116 mL | 109.5290 mL |
| 5 mM | 0.8762 mL | 4.3812 mL | 8.7623 mL | 21.9058 mL | |
| 10 mM | 0.4381 mL | 2.1906 mL | 4.3812 mL | 10.9529 mL | |
| 15 mM | 0.2921 mL | 1.4604 mL | 2.9208 mL | 7.3019 mL | |
| 20 mM | 0.2191 mL | 1.0953 mL | 2.1906 mL | 5.4765 mL | |
| 25 mM | 0.1752 mL | 0.8762 mL | 1.7525 mL | 4.3812 mL | |
| 30 mM | 0.1460 mL | 0.7302 mL | 1.4604 mL | 3.6510 mL | |
| 40 mM | 0.1095 mL | 0.5476 mL | 1.0953 mL | 2.7382 mL | |
| 50 mM | 0.0876 mL | 0.4381 mL | 0.8762 mL | 2.1906 mL | |
| 60 mM | 0.0730 mL | 0.3651 mL | 0.7302 mL | 1.8255 mL | |
| 80 mM | 0.0548 mL | 0.2738 mL | 0.5476 mL | 1.3691 mL | |
| 100 mM | 0.0438 mL | 0.2191 mL | 0.4381 mL | 1.0953 mL |
Ozagrel Related Classifications
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