brinzolamide

Brinzolamide (AL-4862) is a Carbonic Anhydrase Inhibitor. Its mechanism of action involves inhibiting the enzyme Carbonic Anhydrase.

N-desethyl Brinzolamide is an active metabolite of the carbonic anhydrase (CA) inhibitor brinzolamide .1It inhibits CAII and CAIV activities (IC50s = 1.28 and 128 nM, respectively). 1.Kim, C.-Y., Whittington, D.A., Chang, J.S., et al.Structural aspects of isozyme selectivity in the binding of inhibitors to carbonic anhydrases II and IVJ. Med. Chem.45(4)888-893(2002)

O-desmethyl Brinzolamide is an active metabolite of the carbonic anhydrase (CA) inhibitor brinzolamide .1,2It inhibits CAII and CAIV (IC50s = 0.136 and 165 nM, respectively).1 1.Huang, Q., Rui, E.Y., Cobbs, M., et al.Design, synthesis, and evaluation of NO-donor containing carbonic anhydrase inhibitors to lower intraocular pressureJ. Med. Chem.58(6)2821-2833(2015) 2.Lo Faro, A.F., Tini, A., Gottardi, M., et al.Development and validation of a fast ultra-high-performance liquid chromatography tandem mass spectrometry method for determining carbonic anhydrase inhibitors and their metabolites in urine and hairDrug Test Anal.13(8)1552-1560(2021)

Brinzolamide (AL-4862) hydrochloride is a selective inhibitor (IC50: 3.2 nM) of carbonic anhydrase II, inhibiting ciliary CA-II, reducing atrial fluid secretion, and thereby lowering intraocular pressure (IOP). It is useful for studying glaucoma disease.

N-Desethyl Brinzolamide oxalate functions as a dual inhibitor targeting Carbonic anhydrase II and Carbonic anhydrase IV, exhibiting inhibitory concentrations (IC50) of 1.28 nM and 128 nM, respectively [1].

O-Desmethyl Brinzolamide hydrochloride (compound 6a), a potent metabolite derived from Brinzolamide, serves as a carbonic anhydrase (CA) inhibitor. It exhibits a dissociation constant (Kd) of 0.136 nM for CA II and an inhibitory concentration (IC50) of 165 nM for CA IV [1].