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Brinzolamide
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Brinzolamide图片
CAS NO:138890-62-7
包装:50mg
市场价:1134元

产品介绍
Brinzolamide (AL-4862) 是一种选择性碳酸酐酶 II 抑制剂,IC50 值为 3.2 nM。
Cas No.138890-62-7
别名布林佐胺; AL-4862
化学名(4R)-4-(ethylamino)-2-(3-methoxypropyl)-1,1-dioxo-3,4-dihydrothieno[3,2-e]thiazine-6-sulfonamide
Canonical SMILESO=S(C(S1)=CC2=C1S(N(CCCOC)C[C@@H]2NCC)(=O)=O)(N)=O
分子式C12H21N3O5S3
分子量383.51
溶解度≥ 15.05 mg/mL in DMSO, ≥ 8.82 mg/mL in EtOH with ultrasonic and warming
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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 pressure [1].

References:
[1] DeSantis L. Preclinical overview of brinzolamide. Surv Ophthalmol. 2000 Jan;44 Suppl 2:S119-29.