Ozagrel Sodium

Alias: Ozagrel Sodium; KCT-0809; KCT 0809; KCT0809; Cataclot Xanbo
Cat No.:V21605 Purity: ≥98%
Ozagrel Sodium (formerly known as KCT-0809 and Cataclot) is the sodium salt of Ozagrel(also known as OKY-046) which is a potent and selective thromboxane A(2) (TXA(2)) synthetase inhibitor with IC50 of 11 nM for rabbit platelet, it is used for the improvement of postoperative cerebrovascular contraction and accompanying cerebral ischaemia.
Ozagrel Sodium Chemical Structure CAS No.: 189224-26-8
Product category: Prostaglandin Receptor
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
25mg
50mg
100mg
250mg
500mg
1g
2g
Other Sizes

Other Forms of Ozagrel Sodium:

  • Ozagrel
  • Ozagrel HCl (OKY046 HCl; KCT0809; Cataclot)
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Ozagrel Sodium (formerly known as KCT-0809 and Cataclot) is the sodium salt of Ozagrel (also known as OKY-046) which is a potent and selective thromboxane A(2) (TXA(2)) synthetase inhibitor with IC50 of 11 nM for rabbit platelet, it is used for the improvement of postoperative cerebrovascular contraction and accompanying cerebral ischaemia. Ozagrel inhibits the production of thromboxane A(2) induced by oleic acid (OA), which in turn raises the total protein concentration, neutrophil and macrophage counts in bronchoalveolar lavage fluid, and increases the expression of interleukin-8 mRNA and monocyte chemoattractant protein-1 in the guinea pigs' entire lung.

Biological Activity I Assay Protocols (From Reference)
Targets
TXA2
ln Vitro

In vitro activity: Ozagrel raised 6-keto-PGF1 alpha, one of PGI2's stable metabolites, in a variety of isolated cells and tissues, possibly through PG endoperoxides that accumulated as a result of TXA2 synthase inhibition.

ln Vivo
Ozagrel inhibits the production of thromboxane A(2) induced by oleic acid (OA), which in turn raises the total protein concentration, neutrophil and macrophage counts in bronchoalveolar lavage fluid, and increases the expression of interleukin-8 mRNA and monocyte chemoattractant protein-1 in the guinea pigs' entire lung. Ozagrel (3 mg/kg) reduces the cortical infarction's area and volume in rats following ischemia-reperfusion of the middle cerebral artery. Additionally, obagrel suppresses the neurologic deficits in the rat model of microthrombosis. In the conscious cerebral ischemia-reperfusion mouse model, omeprazole ameliorates the reduced spontaneous locomotor activity and the blockage of motor coordination. Ozagrel recovers the postischemic decrease in cortical PO(2) following middle cerebral artery occlusion-reperfusion in cats and suppresses the decrease in specific gravity of the brain tissue caused by the occlusion-reperfusion in the conscious cerebral ischemia-reperfusion SHR model. Along with improving the reduced spontaneous locomotor activity in the conscious cerebral ischemia-reperfusion mouse model, oxagrel also raises the level of 6-keto-PGF(1alpha), a metabolite of prostaglandin I(2) (PGI(2)), in the brain tissue following cerebral ischemia-reperfusion. In intravenous oxagrel-treated guinea pigs, the decrease in Pao(2) and pulmonary vascular hyper-permeability are prevented 30 minutes prior to oleic acid injection. Additionally, oxagrel prevents increases in the weight ratio of TXB(2) to 6-keto prostaglandin F(1alpha) in guinea pig bronchoalveolar lavage fluid, which is a measure of lung cell injury.
Animal Protocol
3 mg/kg
Guinea pigs
References

[1]. J Pharmacol Sci . 2009 Oct;111(2):211-5.

[2]. Pharmacology . 1999 Nov;59(5):257-65.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C13H11N2NAO2
Molecular Weight
250.2328
Exact Mass
250.07
Elemental Analysis
C, 62.40; H, 4.43; N, 11.20; Na, 9.19; O, 12.79
CAS #
189224-26-8
Related CAS #
Ozagrel; 82571-53-7; Ozagrel hydrochloride; 78712-43-3
Appearance
Solid powder
SMILES
C1=CC(=CC=C1CN2C=CN=C2)/C=C/C(=O)[O-].[Na+]
InChi Key
NCNYJCOBUTXCBR-IPZCTEOASA-M
InChi Code
InChI=1S/C13H12N2O2.Na/c16-13(17)6-5-11-1-3-12(4-2-11)9-15-8-7-14-10-15;/h1-8,10H,9H2,(H,16,17);/q;+1/p-1/b6-5+;
Chemical Name
sodium;(E)-3-[4-(imidazol-1-ylmethyl)phenyl]prop-2-enoate
Synonyms
Ozagrel Sodium; KCT-0809; KCT 0809; KCT0809; Cataclot Xanbo
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
H2O: ~50 mg/mL (~199.8 mM)
DMSO: 1~6.3 mg/mL (4~25 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 0.62 mg/mL (2.48 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 6.2 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: ≥ 0.62 mg/mL (2.48 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 6.2 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.

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Solubility in Formulation 3: 70 mg/mL (279.74 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication.


 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 3.9963 mL 19.9816 mL 39.9632 mL
5 mM 0.7993 mL 3.9963 mL 7.9926 mL
10 mM 0.3996 mL 1.9982 mL 3.9963 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.

Calculator

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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.

Clinical Trial Information
NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT00200356 Completed Drug: Edaravone
Drug: Sodium Ozagrel
Cerebral Infarction Mitsubishi Tanabe Pharma
Corporation
August 2004 Phase 4
Biological Data
  • Ozagrel


    Effects of ozagrel on serum ALT level and survival rate in APAP-induced liver injury.BMC Gastroenterol. 2013; 13: 21.

  • Ozagrel

    Effects of ozagrel on hepatic cell death-related markers in liver induced by APAP injection.BMC Gastroenterol. 2013; 13: 21.


  • Ozagrel

    Effects of ozagrel on hepatic GSH depletion induced by APAP and CYP 2E1 level.BMC Gastroenterol. 2013; 13: 21.
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