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CAS NO.138890-62-7
Top quality BrinzolaMide manufacturer in China
Brinzolamide is a specific carbonic anhydrase (CA) inhibitor specifically carbonic anhydrase II. It lowers intraocular pressure (IOP) by reducing the rate of aqueous humor formation (AHF).
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.
Product Number | B4258 |
Purity / Analysis Method | >98.0%(HPLC) |
Molecular Formula / Molecular Weight | C12H21N3O5S3 = 383.50 |
Physical State (20 deg.C) | Solid |
Storage Temperature | <0°C |
Condition to Avoid | Heat Sensitive |
CAS RN | 138890-62-7 |
Reaxys Registry Number | 9651552 |
PubChem Substance ID | 253660292 |
Merck Index (14) | 1376 |
MDL Number |
MFCD08067749 |
Brinzolamide is a potent and selective inhibitor of carbonic anhydrase type II (CA II) with IC50 value of 3.19nM [1].
Brinzolamide is the newest topical CAI to be successfully developed and marketed. It is a safe and efficacious glaucoma drug. In the in vitro assay, brinzolamide has its highest affinity (Ki of 0.13nM) and inhibitory potency (IC50 of 3.19 nM) for CA-II. It has much higher affinity and greater potency for CA-II than for CA-I and CAIV. In the in vivo models, administration of brinzolamide significantly reduces the intraocular pressure (IOP) both in the pigmented rabbits and cynomolgus monkeys with ocular hypertension induced by argon laser trabeculoplasty [1].
As an inhibitor of CA, brinzolamide is also used to assess cerebral blood flow reserve as it can conserve CO2 in the tissues, and the CO2 can then act on blood vessels and produce vasodilatation. Moreover, brinzolamide is proved to be safe and efficacious for reducing intraocular pressur
Product Name |
Brinzolamide |
|
CAS Registry Number | 138890-62-7 | |
Molecular Formula | C12H21N3O5S3 | |
Molecular Weight | 383.51 |