Size | Price | Stock | Qty |
---|---|---|---|
10mg |
|
||
25mg |
|
||
50mg |
|
||
100mg |
|
||
250mg |
|
||
Other Sizes |
|
Purity: ≥98%
Brinzolamide (AL-4862; AL4862; Azopt, Alcon Laboratories, Befardin, AL4862) is a highly potent and selective CAI (carbonic anhydrase II inhibitor) with anti-hypertensive activity. It inhibits carbonic anhydrase II with an IC50 of 3.19 nM. Brinzolamide is used to treat glaucoma (open angle-type) or other eye diseases (e.g. ocular hypertension).
ln Vitro |
|
|
---|---|---|
ln Vivo |
In normotensive NZW rabbits, brinzolamide (7.5 mg or 12 mg) implanted in a silicone matrix is incredibly well tolerated, resulting in prolonged release of the drug and a notable drop in intraocular pressure (IOP) for up to 28 days[2]. No negative effects or toxic symptoms are observed. The parameters of Brinzolamide's pharmacokinetics in rabbits[1]. Topical Administration (500 mg) Topical Administration (500 mg) PK Parameters Aqueous Humor Iris-Ciliary Body Aqueous Humor Iris-Ciliary Body Tmax (h) 0.08 0.5 1 0.25 Cmax (ng/mL, ng/g) 11,050 1964 408 1245 Terminal t1/2 (h) 3.4 13 2 13.6 AUC0-24h (h*ng/mL, h*ng/g) 17,780 7725 1896 11414 AUC0-∞ (h*ng/mL, h*ng/g) 17,836 8839 1955 16628 Dose-normalized AUC0-∞ (h*/mL, h*/g) 4 2 0.004 0.03
|
|
Animal Protocol |
Animal/Disease Models: Rabbits [2]
Doses: 7.5 mg, 12 mg Route of Administration: Brinzolamide silicone matrix implant placed in the episcleral space Experimental Results: Resulted in a significant IOP reduction of 4.6 mmHg on days 10-28, with concentrations of 12 mg. |
|
References |
[1]. Vatsala Naageshwaran, et al. Comprehensive Ocular and Systemic Pharmacokinetics of Brinzolamide in Rabbits After Intracameral, Topical, and Intravenous Administration. J Pharm Sci. 2021 Jan;110(1):529-535.
[2]. Sara M.Smith, et al. Tolerability, pharmacokinetics, and pharmacodynamics of a brinzolamide episcleral sustained release implant in normotensive New Zealand white rabbits,Journal of Drug Delivery Science and Technology,Volume 61,2021,102123,ISSN 1773-224 |
Molecular Formula |
C12H21N3O5S3
|
---|---|
Molecular Weight |
383.51
|
CAS # |
138890-62-7
|
Related CAS # |
Brinzolamide hydrochloride;150937-43-2;Brinzolamide-d5;1217651-02-9
|
Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
|
SMILES |
O=S(C(S1)=CC2=C1S(N(CCCOC)C[C@@H]2NCC)(=O)=O)(N)=O
|
Synonyms |
AL 4862; Brinzolamide; trade names Azopt, Alcon Laboratories, Befardin, Fardi Medicals; AL-4862; AL4862
|
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 (In Vitro) |
|
|||
---|---|---|---|---|
Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.75 mg/mL (7.17 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 27.5 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: ≥ 2.75 mg/mL (7.17 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 27.5 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. View More
Solubility in Formulation 3: ≥ 2.75 mg/mL (7.17 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.6075 mL | 13.0375 mL | 26.0749 mL | |
5 mM | 0.5215 mL | 2.6075 mL | 5.2150 mL | |
10 mM | 0.2607 mL | 1.3037 mL | 2.6075 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.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT03896633 | Completed Has Results | Drug: brinzolamide 1% ophthalmic suspension |
Glaucoma Open Angle or Ocular Hypertension |
Bausch & Lomb Incorporated | February 28, 2018 | Phase 1 Phase 2 |
NCT04523844 | Completed | Drug: Brinzolamide-brimonidine Fixed Combination |
Eye Diseases Injection Complication |
General Hospital of Athens Elpis | May 11, 2020 | Not Applicable |
NCT03494257 | Completed | Drug: Brinzolamide-Brimonidine fixed combination |
Cataract Intraocular Pressure |
University Hospital of Patras | September 4, 2017 | Not Applicable |
NCT01721707 | Withdrawn | Drug: Latanoprost+Brinzolamide combination |
Open Angle Glaucoma Ocular Hypertension |
Adapt Produtos Oftalmológicos Ltda. | December 2012 | Phase 3 |