Brinzolamide

Catalog No.S3178 Synonyms: AL-4862

Brinzolamide Chemical Structure

Molecular Weight(MW): 383.51

Brinzolamide is a potent carbonic anhydrase II inhibitor with IC50 of 3.19 nM.

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In DMSO USD 90 In stock
USD 70 In stock
USD 270 In stock
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Biological Activity

Description Brinzolamide 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

Solubility (25°C)

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

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 383.51
Formula

C12H21N3O5S3

CAS No. 138890-62-7
Storage powder
Synonyms AL-4862

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02419508 Recruiting Open-Angle Glaucoma|Ocular Hypertension Alcon Research August 7, 2015 Phase 4
NCT02730871 Recruiting Open-angle Glaucoma|Ocular Hypertension Alcon Research June 2016 Phase 4
NCT02770248 Completed Glaucoma Alcon Research May 2016 Phase 4
NCT02512042 Completed Glaucoma Actavis Inc. April 2015 Phase 3
NCT02339584 Completed Open-Angle Glaucoma|Ocular Hypertension Alcon Research April 2015 Phase 3
NCT02325518 Completed Open-Angle Glaucoma|Ocular Hypertension Alcon, a Novartis Company|Alcon Research December 2014 Phase 4

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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.

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Carbonic Anhydrase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID