Brinzolamide

Alias: AL 4862; Brinzolamide; trade names Azopt, Alcon Laboratories, Befardin, Fardi Medicals; AL-4862; AL4862
Cat No.:V0898 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.
Brinzolamide Chemical Structure CAS No.: 138890-62-7
Product category: Carbonic Anhydrase
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 Brinzolamide:

  • Brinzolamide HCl
  • Brinzolamide-d5 (AL-4862-d5)
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

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).

Biological Activity I Assay Protocols (From Reference)
ln Vitro

In vitro activity: Brinzolamide is the newest topical CAI to be successfully developed and marketed. It is a safe and efficacious glaucoma drug. In the in vitro assay, brinzolamide has its highest affinity (Ki of 0.13nM) and inhibitory potency (IC50 of 3.19 nM) for CA-II. It has much higher affinity and greater potency for CA-II than for CA-I and CAIV. In the in vivo models, administration of brinzolamide significantly reduces the intraocular pressure (IOP) both in the pigmented rabbits and cynomolgus monkeys with ocular hypertension induced by argon laser trabeculoplasty.


Kinase Assay: Brinzolamide(AL 4862) is a potent carbonic anhydrase II inhibitor with IC50 of 3.19 nM.

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
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C12H21N3O5S3
Molecular Weight
383.51
CAS #
138890-62-7
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
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: 77 mg/mL (200.8 mM)
Water:< 1 mg/mL
Ethanol:< 1 mg/mL
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.

Calculator

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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)
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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.
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Biological Data
  • Brinzolamide

    Changes in IOP over 24 hours after brinzolamide administration. (a) Brinzolamide-treated eye. (b) Brinzolamide-untreated eye.Open Ophthalmol J. 2008; 2: 160–164.
  • Brinzolamide

    Percent reduction in IOPs over 24 hours after brinzolamide administration.Open Ophthalmol J. 2008; 2: 160–164.
  • Brinzolamide

    Difference in IOP between right and left eyes before and after brinzolamide administration.Open Ophthalmol J. 2008; 2: 160–164.
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