- U-104
- Methazolamide
- Topiramate
- Tioxolone
- Dorzolamide HCl
| BrinzolamideCA II inhibitor |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
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- Purity = 99.88%
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Chemical structure
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| Cas No. | 138890-62-7 | SDF | Download SDF |
| Synonyms | N/A | ||
| Chemical Name | (4R)-4-(ethylamino)-2-(3-methoxypropyl)-1,1-dioxo-3,4-dihydrothieno[3,2-e]thiazine-6-sulfonamide | ||
| Canonical SMILES | O=S(C(S1)=CC2=C1S(N(CCCOC)C[C@@H]2NCC)(=O)=O)(N)=O | ||
| Formula | C12H21N3O5S3 | M.Wt | 383.51 |
| Solubility | ≥15.05 mg/mL in DMSO, ≥8.82 mg/mL in EtOH with ultrasonic and warming, <2.25 mg/ml="" in="" h2o=""> | Storage | Store at -20°C |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
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.
