| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Pirenoxine's mode of action involves antioxidant and anti-inflammatory properties, which help in reducing oxidative stress and inflammation in the eye tissues. It is believed to inhibit the formation of cataracts by preventing protein denaturation and aggregation in the lens. Pirenoxine interacts with selenite and calcium ions implicated in cataractogenesis. It also aids in maintaining proper eye lubrication by enhancing tear film stability.
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| ln Vitro |
Pirenoxine is a potent antioxidant. It demonstrates antioxidant properties and interacts with selenite and calcium ions. The compound has anti-cataractogenesis activity by interacting with calcium ions or selenite which could lead to the formation of lens cataract. Specific IC50 or EC50 values for its antioxidant or anti-cataract activities are not extensively detailed in standard reference sources.
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| ln Vivo |
Lens tumors are inhibited and presbyopia is prevented by pirenoxine (0.005% pirenoxine; eye drops) [2].
Pirenoxine (0.005% pirenoxine; eye drops) inhibits lens hardening and prevents the development of presbyopia. It has been used in clinical practice as an eye drop for the treatment of cataracts. In vivo studies in animal models of cataract have demonstrated its efficacy in preventing or delaying cataract formation. |
| Enzyme Assay |
Pirenoxine's antioxidant activity can be assessed using standard in vitro assays such as the DPPH radical scavenging assay, ABTS radical cation decolorization assay, or ferric reducing antioxidant power (FRAP) assay. The compound's ability to prevent protein aggregation can be studied using lens protein solutions (e.g., α-crystallin) exposed to oxidative stress or calcium ions. The extent of protein aggregation is measured by turbidity (absorbance at 360 nm) or by light scattering.
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| Cell Assay |
The anti-cataract activity of pirenoxine is evaluated in vitro using lens epithelial cells (e.g., human lens epithelial cells, HLEC) or rat lens organ cultures. Cells or lenses are treated with cataract-inducing agents such as selenite, calcium ionophore, or hydrogen peroxide in the presence or absence of pirenoxine. Cell viability, oxidative stress markers (e.g., ROS, MDA), and lens opacity are measured to assess the protective effects of the compound.
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| Animal Protocol |
Animal/Disease Models: Sixweeks old male SD (SD (Sprague-Dawley)) rats [2]
Doses: 0.005% pirenoxine Route of Administration: eye drops Experimental Results: Dramatically inhibited lens hardening. Pirenoxine is typically administered as eye drops in animal models of cataract. In selenite-induced cataract models in rats, Pirenoxine eye drops (0.005%) are administered topically multiple times daily. Lens opacity is graded using a slit-lamp microscope, and biochemical parameters such as lens malondialdehyde (MDA) and glutathione levels are measured. The progression of lens hardening is assessed to evaluate anti-presbyopic activity. |
| ADME/Pharmacokinetics |
Pirenoxine is very soluble in water. Specific pharmacokinetic parameters such as absorption, distribution, metabolism, and excretion are not extensively detailed for ophthalmic administration. As an eye drop, it is expected to act locally in the eye with minimal systemic absorption.
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| Toxicity/Toxicokinetics |
Pirenoxine has a favorable toxicity profile. The oral LD50 in mice is >10000 mg/kg; subcutaneous LD50 is >5000 mg/kg; intraperitoneal LD50 is 2120-2250 mg/kg. The intraperitoneal LD50 in rats is also available. These data indicate low acute toxicity.
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| References | |
| Additional Infomation |
Pyrenoxine is an organic molecular entity.
Pirenoxine (CAS# 1043-21-6) is also known by its trade names Catalin® and Kary Uni®. Regulatory-grade pirenoxine is manufactured by Senju Pharmaceutical Co., Ltd. The compound has been used clinically as an eye drop for cataract treatment in several countries. It has potential for cataract research and is a well-established compound in ophthalmic pharmacology. |
| Molecular Formula |
C16H8N2O5
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|---|---|
| Molecular Weight |
308.25
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| Exact Mass |
308.043
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| CAS # |
1043-21-6
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| Related CAS # |
1043-21-6;51410-30-1 (salt);
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| PubChem CID |
4846
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| Appearance |
Light brown to brown solid powder
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| Density |
1.7g/cm3
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| Boiling Point |
515.8ºC at 760mmHg
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| Melting Point |
247-248ºC
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| Flash Point |
265.7ºC
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| Vapour Pressure |
1.83E-11mmHg at 25°C
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| Index of Refraction |
1.793
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| LogP |
2.244
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
23
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| Complexity |
771
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
OKPNYGAWTYOBFZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H8N2O5/c19-9-5-8(16(21)22)18-14-10(20)6-12-15(13(9)14)17-7-3-1-2-4-11(7)23-12/h1-6H,(H,18,19)(H,21,22)
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| Chemical Name |
1,5-dioxo-4H-pyrido[3,2-a]phenoxazine-3-carboxylic acid
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| Synonyms |
Pirenoxine Catalin PRX
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO :< 1 mg/mL
H2O : < 0.1 mg/mL |
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2441 mL | 16.2206 mL | 32.4412 mL | |
| 5 mM | 0.6488 mL | 3.2441 mL | 6.4882 mL | |
| 10 mM | 0.3244 mL | 1.6221 mL | 3.2441 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.
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.
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