2. GPCR/G Protein
  3. Prostaglandin Receptor
  4. Ozagrel

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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Ozagrel

Ozagrel 構造式

CAS 番号 : 82571-53-7

容量 価格（税別） 在庫状況 数量
>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 36 在庫あり
Solution
10 mM * 1 mL in DMSO USD 36 在庫あり
Solid
5 mg $33 在庫あり
10 mg $49 在庫あり
25 mg $88 在庫あり
50 mg $133 在庫あり
100 mg $200 在庫あり
200 mg   お問い合わせ  
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* アイテムを追加する前、数量をご選択ください

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Based on 1 publication(s) in Google Scholar

Other Forms of Ozagrel:

Ozagrel 関連抗体

Top Publications Citing Use of Products

Prostaglandin Receptor アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
DP EP FP IP TXA2/TP TXB2

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  • 純度とドキュメンテーション

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製品説明

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[1][2][3][4][5].

IC50 & Target[1][5]

TXA2/TP

11 nM ()

TXB2

 

Cellular Effect
Cell Line Type Value Description References
Platelet IC50
0.36 mM
Compound: Ozagrel
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
[PMID: 21993151]
Platelet IC50
0.36 mM
Compound: Ozagrel
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
10.1039/C3MD20352B
Platelet IC50
144.1 μM
Compound: Ozagrel
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
10.1039/C4MD00022F
Platelet IC50
2.85 mM
Compound: Ozagrel
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
[PMID: 34902735]
Platelet IC50
53.1 μM
Compound: Ozagrel
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
[PMID: 28453995]
体外実験

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 関連抗体
体内実験

Ozagrel (10-20 mg/kg, p.o., once daily for 6-21 days) markedly improves extenuates endothelial dysfunction, oxidative stress and neuroinflammation in rat model of bilateral common carotid artery occlusion induced by L-Methionine (HY-N0326) and bilateral common carotid artery occlusion (BCCAo)[2][3].
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.

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]
Dosage: 10 and 20 mg/kg
Administration: Oral administration (p.o.), once daily for 21 days
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.
Animal Model: BCCAo induced vascular dementia (VaD) model established in Wistar rats of both sex and weighing 200 g[3]
Dosage: 10 and 20 mg/kg
Administration: Oral administration (p.o.), once daily for 6 days
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.
Animal Model: OA-induced lung Injury model established in male Hartley guinea pigs (420-500 g) [4]
Dosage: 80 mg/kg
Administration: Intravenous injection (i.v.), single dose, 3 h after OA injection
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.
分子量

228.25

分子式

C13H12N2O2
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

O=C(O)/C=C/C1=CC=C(CN2C=CN=C2)C=C1
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.3812 mL 21.9058 mL 43.8116 mL
5 mM 0.8762 mL 4.3812 mL 8.7623 mL
10 mM 0.4381 mL 2.1906 mL 4.3812 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

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体積 （開始）

V1

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濃度 （終了）

C2

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体積 （終了）

V2

体内:

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.

  • Protocol 1

    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.
  • Protocol 2

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

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(per animal)

g

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(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
純度とドキュメンテーション
参考文献

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
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Ozagrel Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Ozagrel82571-53-7OKY-046OKY046OKY 046Prostaglandin ReceptorThromboxane-A2Oxidative stressMemoryVascular DementiaAntihemostaticAntiplateletInhibitorinhibitorinhibit

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製品名:
Ozagrel
製品番号:
HY-B0428
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