Ozagrel is a synthetic thromboxane A₂ synthase inhibitor used as an antiplatelet and antithrombotic pharmaceutical agent. The pharmaceutical API is commonly supplied as Ozagrel Sodium, the sodium salt of ozagrel. Ozagrel sodium is particularly associated with pharmaceutical preparations used in Japan for the management of cerebral ischemic conditions.
Ozagrel itself has the molecular formula C₁₃H₁₂N₂O₂, CAS Number 82571-53-7, and molecular weight 228.25 g/mol. The sodium salt has the formula C₁₃H₁₁N₂NaO₂, CAS Number 189224-26-8, and molecular weight 250.23 g/mol. PubChem confirms these identities and identifies ozagrel sodium as the sodium salt of ozagrel.
Ozagrel Sodium is chemically designated as Monosodium (2E)-3-[4-(1H-imidazol-1-ylmethyl)phenyl]prop-2-enoate. The API occurs as white crystals or crystalline powder. According to JP XVIII, it is freely soluble in water, soluble in methanol and practically insoluble in ethanol (99.5).
The sodium salt is the form most relevant to pharmaceutical API manufacturing and injectable drug products. It should therefore be clearly differentiated from free ozagrel and from ozagrel hydrochloride.
Ozagrel is a selective thromboxane A₂ synthase inhibitor. Thromboxane A₂ is involved in platelet aggregation and vasoconstriction. By inhibiting thromboxane A₂ synthesis, ozagrel influences platelet aggregation and vascular responses.
Ozagrel sodium has been used in pharmaceutical products associated with cerebral ischemic disorders. PubChem classifies ozagrel among enzyme inhibitors and fibrinolytic-related pharmacological substances, while chemical and pharmaceutical literature identifies its principal activity as thromboxane A₂ synthase inhibition.
Ozagrel Sodium is particularly associated with pharmaceutical preparations for cerebral ischemic conditions and antiplatelet therapy.
Applications include:
Japanese Pharmacopoeia includes separate monographs for Ozagrel Sodium, Ozagrel Sodium Injection, and Ozagrel Sodium for Injection, demonstrating the established pharmaceutical use of the sodium salt.
Ozagrel Sodium has a molecular weight of 250.23 g/mol and molecular formula C₁₃H₁₁N₂NaO₂. Its chemical structure contains an imidazole ring connected through a methylene group to a substituted phenyl ring and an E-configured acrylic-acid sodium salt.
The verified IUPAC name is:
Sodium (E)-3-[4-(imidazol-1-ylmethyl)phenyl]prop-2-enoate
PubChem assigns Ozagrel Sodium CID 23663942, while its KEGG identifier is D01684 and FDA UNII is 4X5577N3ET.
The JP XVIII official monograph provides particularly useful numerical quality criteria for Ozagrel Sodium. When dried, the API contains 98.0–102.0% of Ozagrel Sodium. The monograph therefore provides a reliable pharmacopoeial assay range for CMS documentation.
The JP monograph also specifies a pH of 9.5–10.5, measured using 0.5 g of Ozagrel Sodium dissolved in 10 mL of water.
For chloride, the limit is NMT 0.012%, equivalent to NMT 120 ppm. Heavy metals are controlled at NMT 10 ppm.
Related substances are controlled using liquid chromatography. According to JP XVIII, each impurity other than ozagrel is limited to NMT 0.2%, while the total amount of impurities other than ozagrel is limited to NMT 0.5%.
A 2023 study from the Shanghai Institute for Food and Drug Control also investigated related substances in marketed Ozagrel Sodium injection products using HPLC. Forty-six batches were examined; total impurities in all tested samples were below 1.0%, while the highest individual impurity in five samples ranged from 0.16–0.23%. This study supports the importance of comprehensive impurity monitoring but should not replace the official JP release limits.
JP XVIII uses liquid chromatography for the assay of Ozagrel Sodium. The method uses UV detection at 272 nm, an ODS column measuring 4.6 mm × 15 cm with 5 µm packing, and an ammonium acetate/methanol mobile phase. The flow rate is adjusted so that the ozagrel retention time is approximately 10 minutes.
For related substances, the JP method uses UV detection at 220 nm. The same chromatographic column, column temperature, mobile phase and flow rate are used as specified under the assay conditions. System suitability requires a theoretical plate count of NLT 6000, symmetry factor NMT 2.0, and repeatability RSD NMT 2.0%.
JP XVIII specifies NMT 0.5% loss on drying for Ozagrel Sodium. The test is performed on 1 g at 105°C for 4 hours. This is a strong numerical value for your CMS because it comes directly from the current official JP XVIII monograph.
Ozagrel Sodium occurs as white crystals or crystalline powder. It is freely soluble in water, soluble in methanol, and practically insoluble in ethanol (99.5) according to JP XVIII.
A commercial analytical reference product from TCI reports the same molecular formula and molecular weight and identifies the material as a solid. TCI reports an analytical purity of >98.0% by HPLC for its research-grade material, but this should not be substituted for the official JP pharmaceutical assay range.
JP XVIII specifies tight containers and light-resistant storage for Ozagrel Sodium. These conditions should be reflected in technical documentation where the API is represented according to the JP standard.
Ozagrel Sodium is also recognized in JP XVIII as an injectable pharmaceutical preparation. The monograph for Ozagrel Sodium Injection specifies 95.0–105.0% of the labeled amount, while bacterial endotoxins are specified at less than 3.7 EU/mg. These are requirements for the finished injection, not the bulk API, and should therefore not be placed in the API specification table.
Ozagrel API manufacturing requires controlled synthesis, purification, drying and analytical release testing. For pharmaceutical-grade Ozagrel Sodium, appropriate quality control includes identity testing, HPLC assay, related-substance testing, pH, chloride, heavy metals and loss on drying.
For a CMS/API page, Ozagrel Sodium should be the principal product name if the material being offered is CAS 189224-26-8. The free acid Ozagrel, CAS 82571-53-7, should be treated as a separate chemical form. PubChem confirms the distinction between the parent compound and sodium salt.
| Parameter | Specification |
|---|---|
| Appearance | white to off-white crystalline powder |
| Identification | IR & HPLC compliant0.5 |
| Assay (HPLC) | 98.0% – 102.0% |
| Loss on Drying | NMT 0.5% |
| Heavy Metals | NMT 10 ppm |
| pH (1% Solution) | 9.5–10.5 |
| Individual Impurity | NMT 0.5% |