Ozagrel HCl (OKY046 HCl; KCT0809; Cataclot)

Alias: OKY-046 HCl;KCT 0809;Cataclot; Xanbo;OKY046 HCl;Ozagrel hydrochloride, Ozagrel HCl;OKY 046 HCl;Ozagrel; KCT-0809; KCT0809; Ozagrel free acid
Cat No.:V0817 Purity: ≥98%
Ozagrel HCl(OKY-046 HCl;KCT 0809;Cataclot; Xanbo;OKY046 HCl), the hydrochloride salt of the antiplatelet drug Ozagrel, is a selective inhibitor of thromboxane A(2) (TXA(2)) synthetase (IC50 = 11 nM) with potential use for for the improving postoperative cerebrovascular contraction and accompanying cerebral ischaemia.
Ozagrel HCl (OKY046 HCl; KCT0809; Cataclot) Chemical Structure CAS No.: 78712-43-3
Product category: P450 (e.g. CYP)
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
10mg
25mg
50mg
100mg
250mg
Other Sizes

Other Forms of Ozagrel HCl (OKY046 HCl; KCT0809; Cataclot):

  • Ozagrel
  • Ozagrel Sodium
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Ozagrel HCl (OKY-046 HCl; KCT 0809; Cataclot; Xanbo; OKY046 HCl), the hydrochloride salt of the antiplatelet drug Ozagrel, is a selective inhibitor of thromboxane A(2) (TXA(2)) synthetase (IC50 = 11 nM) with potential use for for the improving postoperative cerebrovascular contraction and accompanying cerebral ischaemia. Ozagrel prevents oleic acid (OA) induced thromboxane A(2) generation and subsequently increased total protein concentration and the numbers of macrophages and neutrophils in bronchoalveolar lavage fluid and increased monocyte chemoattractant protein-1 andinterleukin-8 mRNA expression in the whole lung of guinea pigs.

Biological Activity I Assay Protocols (From Reference)
ln Vitro

In vitro activity: Ozagrel(OKY-046) is an antiplatelet agent working as a thromboxane A2 synthesis inhibitor. Ozagrel was selected as the best compound of highly selective inhibitors of TXA2 synthase. The inhibition of TXA2 synthase by ozagrel was more effective on human and rabbit enzymes than those of other species. Ozagrel increased 6-keto-PGF1 alpha, one of stable metabolites of PGI2, in various isolated cells and tissues perhaps via accumulated PG endoperoxides resulted by the inhibition of TXA2 synthase

ln Vivo
Ozagrel prevents oleic acid (OA) induced thromboxane A(2) generation and subsequently increased total protein concentration and the numbers of macrophages and neutrophils in bronchoalveolar lavage fluid and increased monocyte chemoattractant protein-1 andinterleukin-8 mRNA expression in the whole lung of guinea pigs. Ozagrel (3 mg/kg) decreases both the area and volume of the cortical infarction after ischemia-reperfusion of the middle cerebral artery in rat. Ozagrel also has suppressive effects on the neurologic deficits in the microthrombosis rat model. Ozagrel improves the reduced spontaneously locomotor activity and the obstruction of motor coordination in the conscious cerebral ischemia-reperfusion mouse model. Ozagrel suppresses the decrease in specific gravity of the brain tissue induced by the occlusion-reperfusion in the conscious cerebral ischemia-reperfusion SHR model, and recovers the postischemic decrease in cortical PO(2) after middle cerebral artery occlusion-reperfusion in cats. Ozagrel also increases the level of 6-keto-PGF(1alpha), a metabolite of prostaglandin I(2) (PGI(2)), in the brain tissue after cerebral ischemia-reperfusion, and the administration of PGI(2) improves the reduced spontaneous locomotor activity in the conscious cerebral ischemia-reperfusion mouse model. Ozagrel administered intravenously 30 min before oleic acid injection prevents the decrease in Pao(2) and pulmonary vascular hyper-permeability in guinea-pigs. Ozagrel also prevents increases in lactate dehydrogenase activity, a measure of lung cell injury, TXB(2) and its weight ratio to 6-keto prostaglandin F(1alpha) in bronchoalveolar lavage fluid in guinea-pigs.
Animal Protocol
3 mg/kg
Rats
References
J Pharmacol Sci.2009 Oct;111(2):211-5;Pharmacology.1999 Nov;59(5):257-65.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C13H12N2O2.HCL
Molecular Weight
264.71
CAS #
78712-43-3
Related CAS #
Ozagrel;82571-53-7;Ozagrel sodium;189224-26-8
SMILES
Cl[H].O([H])C(/C(/[H])=C(\[H])/C1C([H])=C([H])C(=C([H])C=1[H])C([H])([H])N1C([H])=NC([H])=C1[H])=O
Synonyms
OKY-046 HCl;KCT 0809;Cataclot; Xanbo;OKY046 HCl;Ozagrel hydrochloride, Ozagrel HCl;OKY 046 HCl;Ozagrel; KCT-0809; KCT0809; Ozagrel free acid
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)
DMSO: 53 mg/mL (200.2 mM)
Water:53 mg/mL (200.2 mM)
Ethanol: 6 mg/mL (22.7 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.86 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 20.8 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: ≥ 2.08 mg/mL (7.86 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 20.8 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: ≥ 2.08 mg/mL (7.86 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.


Solubility in Formulation 4: 25 mg/mL (94.44 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 3.7777 mL 18.8886 mL 37.7772 mL
5 mM 0.7555 mL 3.7777 mL 7.5554 mL
10 mM 0.3778 mL 1.8889 mL 3.7777 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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  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

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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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
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
Instructions to calculate molar mass (molecular weight) of a chemical compound:
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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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.

Biological Data
  • Ozagrel HCl


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


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


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