Brinzolamide

Brinzolamide is a potent inhibitor of carbonic anhydrase II (CAII) and CAIV (IC50s = 3.19 and 45.3 nM, respectively). It is selective for CAII and CAIV over CAI (IC50 = ~1,365 nM). Brinzolamide (30 mg/kg) reduces intestinal charcoal meal progression by 44% and prolongs pentobarbital sodium-induced sleep time by 35% in mice. Topical administration of brinzolamide (0.25, 0.5, and 1 mg/eye) reduces intraocular pressure (IOP) in a rabbit model of spontaneous ocular hypertension. It also reduces IOP in a cynomolgus monkey model of argon laser trabeculoplasty-induced ocular hypertension. Formulations containing brinzolamide have been used in the treatment of glaucoma and ocular hypertension.Formal Name: 4R-(ethylamino)-3,4-dihydro-2-(3-methoxypropyl)-1,1-dioxide-2H-thieno[3,2-e]-1,2-thiazine-6-sulfonamide. CAS Number: 138890-62-7. Synonyms: AL 4862. Molecular Formula: C12H21N3O5S3. Formula Weight: 383.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, DMSO:PBS(pH 7.2) (1:2): 0.3 mg/ml. lambdamax: 253 nm. SMILES: O=S(C1=CC2=C(S1)S(N(CCCOC)C[C@@H]2NCC)(=O)=O)(N)=O. InChi Code: InChI=1S/C12H21N3O5S3/c1-3-14-10-8-15(5-4-6-20-2)23(18,19)12-9(10)7-11(21-12)22(13,16)17/h7,10,14H,3-6,8H2,1-2H3,(H2,13,16,17)/t10-/m0/s1. InChi Key: HCRKCZRJWPKOAR-JTQLQIEISA-N.