Brinzolamide

SKU: orb1226386

Description

Brinzolamide is a highly specific, non-competitive, reversible carbonic anhydrase inhibitor. Carbonic anhydrase (CA) is an enzyme found in many tissues of the body including the eye. It catalyzes the reversible reaction involving the hydration of carbon dioxide and the dehydration of carbonic acid. In humans, carbonic anhydrase exists as a number of isoenzymes, the most active being carbonic anhydrase II (CA-II). Inhibition of carbonic anhydrase in the ciliary processes of the eye decreases aqueous humor secretion, presumably by slowing the formation of bicarbonate ions with subsequent reduction in sodium and fluid transport. The result is a reduction in intraocular pressure. Brinzolamide is indicated in the treatment of elevated intraocular pressure in patients with ocular hypertension or open-angle glaucoma. (In Vivo):Brinzolamide (7.5 mg or 12 mg) implanted in a silicone matrix is extremely well tolerated and provides sustained release of brinzolamide and significant reduction in intraocular pressure (IOP) for up to 28 days with no adverse effects or signs of toxicity in normotensive NZW rabbits.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 138890-62-7
• MW: 383.51
• Purity: >98% (HPLC)
• Formula: C₁₂H₂₁N₃O₅S₃
• SMILES: CCN[C@H]1CN(S(=O)(=O)C2=C1C=C(S2)S(=O)(=O)N)CCCOC
• Target: Carbonic Anhydrase
• Solubility: DMSO: 77 mg/mL (200.77 mM)

Bioactivity

• In Vivo:
  Brinzolamide (7.5 mg or 12 mg) implanted in a silicone matrix is extremely well tolerated and provides sustained release of brinzolamide and significant reduction in intraocular pressure (IOP) for up to 28 days with no adverse effects or signs of toxicity in normotensive NZW rabbits. The pharmacokinetic parameters of Brinzolamide in rabbits. Animal model: Rabbits. Dosage: 7.5 mg, 12 mg. Administration: Brinzolamide silicone matrix implant placed in the episcleral space. Result: Resulted in a significant IOP reduction of 4.6 mmHg on days 10-28, with concentrations of 12 mg.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

AL 4862 | Azopt

Quick Database Links

Gene Symbol

Carbonic Anhydrase