Brinzolamide

Catalog No.S3178 Synonyms: AL-4862

For research use only.

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

Brinzolamide Chemical Structure

CAS No. 138890-62-7

Selleck's Brinzolamide has been cited by 2 Publications

Purity & Quality Control

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Biological Activity

Description Brinzolamide (AL-4862) is a potent carbonic anhydrase II inhibitor with IC50 of 3.19 nM.
Targets
CAII [1]
3.19 nM
In vivo Brinzolamide (< 1 mg) ophthalmic suspension lowers intraocular pressure in Dutch-belted pigmented rabbits in a dose-dependent manner with an onset within 0.5 hour and a peak response by 1–2 hours. Brinzolamide (0.6 mg) ophthalmic suspension lowers intraocular pressure in laser-treated glaucomatous cynomolgus monkeys in a dose-dependent manner with an onset within 1 hour and a peak response by 3 hours. Brinzolamide dosages of 30 mg/kg, produces a 44% reduction in intestinal charcoal meal progression, but 1 and 10 mg/kg produced 8% and 18% decreases, respectively, in male CD-1 mice. Brinzolamide of 1 mg/kg, 10 mg/kg, and 30 mg/kg prolongs barbiturate sleep time by 57%, 15%, and 35%, respectively, in male CD-1 mice. [1] Brinzolamide (< 3%) produces significantly greater mean percent intraocular pressure reductions and mean intraocular pressure reductions compared with placebo in patients with primary, open-angle glaucoma or ocular hypertension. The optimal intraocular pressure-lowering concentration of brinzolamide is 1%, brinzolamide 1% is well tolerated by patients with primary open-angle glaucoma or ocular hypertension when administered twice daily. [2] Brinzolamide significantly decreases intraocular pressure and arteriovenous passage time compared with placebo in healthy volunteers. [3] Brinzolamide (2%) increases optic nerve head blood flow and decreases intraocular pressure in tranquilized Dutch-belted rabbits. [4] Brinzolamide (1%) reduces intraocular pressure by reducing aqueous flow and not by affecting aqueous humor drainage in normotensive eyes of rabbits and hypertensive eyes of monkeys. [5]

Protocol (from reference)

Solubility (25°C)

In vitro

DMSO 77 mg/mL
(200.77 mM)
Water Insoluble
Ethanol Insoluble

Chemical Information

Molecular Weight 383.51
Formula

C12H21N3O5S3

CAS No. 138890-62-7
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCNC1CN(S(=O)(=O)C2=C1C=C(S2)S(=O)(=O)N)CCCOC

In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Molarity Calculator

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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