CAS 138890-62-7|Brinzolamide
| Common Name | Brinzolamide | ||
|---|---|---|---|
| CAS Number | 138890-62-7 | Molecular Weight | 383.507 |
| Density | 1.5±0.1 g/cm3 | Boiling Point | 586.0±60.0 °C at 760 mmHg |
| Molecular Formula | C12H21N3O5S3 | Melting Point | / |
| MSDS | ChineseUSA | Flash Point | 308.2±32.9 °C |
Names
| Name | brinzolamide |
|---|---|
| Synonym | More Synonyms |
Brinzolamide BiologicalActivity
| Description | Brinzolamide(AL 4862) is a potent carbonic anhydrase II inhibitor with IC50 of 3.19 nM.Target: carbonic anhydrase IIBrinzolamide (< 1 mg) ophthalmic suspension lowers intraocular pressure in Dutch-belted pigmented rabbits in a dose-dependent manner with an onset within 0.5 hour and a peak response by 1-2 hours. Brinzolamide (0.6 mg) ophthalmic suspension lowers intraocular pressure in laser-treated glaucomatous cynomolgus monkeys in a dose-dependent manner with an onset within 1 hour and a peak response by 3 hours. Brinzolamide dosages of 30 mg/kg, produces a 44% reduction in intestinal charcoal meal progression, but 1 and 10 mg/kg produced 8% and 18% decreases, respectively, in male CD-1 mice. Brinzolamide of 1 mg/kg, 10 mg/kg, and 30 mg/kg prolongs barbiturate sleep time by 57%, 15%, and 35%, respectively, in male CD-1 mice [1]. Brinzolamide (< 3%) produces significantly greater mean percent intraocular pressure reductions and mean intraocular pressure reductions compared with placebo in patients with primary, open-angle glaucoma or ocular hypertension. The optimal intraocular pressure-lowering concentration of brinzolamide is 1%, brinzolamide 1% is well tolerated by patients with primary open-angle glaucoma or ocular hypertension when administered twice daily [2]. |
|---|---|
| Related Catalog | Signaling Pathways >>Metabolic Enzyme/Protease >>Carbonic AnhydraseResearch Areas >>Others |
| References | [1]. DeSantis, L., Preclinical overview of brinzolamide. Surv Ophthalmol, 2000. 44 Suppl 2: p. S119-29. [2]. Silver, L.H., Dose-response evaluation of the ocular hypotensive effect of brinzolamide ophthalmic suspension (Azopt). Brinzolamide Dose-Response Study Group. Surv Ophthalmol, 2000. 44 Suppl 2: p. S147-53. |
Chemical & Physical Properties
| Density | 1.5±0.1 g/cm3 |
|---|---|
| Boiling Point | 586.0±60.0 °C at 760 mmHg |
| Molecular Formula | C12H21N3O5S3 |
| Molecular Weight | 383.507 |
| Flash Point | 308.2±32.9 °C |
| Exact Mass | 383.064331 |
| PSA | 163.80000 |
| LogP | -0.65 |
| Vapour Pressure | 0.0±1.6 mmHg at 25°C |
| Index of Refraction | 1.626 |
| InChIKey | HCRKCZRJWPKOAR-JTQLQIEISA-N |
| SMILES | CCNC1CN(CCCOC)S(=O)(=O)c2sc(S(N)(=O)=O)cc21 |
| Storage condition | ?20°C |
Safety Information
| Hazard Codes | Xi |
|---|---|
| Risk Phrases | R36/37/38:Irritating to eyes, respiratory system and skin . |
| Safety Phrases | S26-S36 |
| RIDADR | NONH for all modes of transport |
| RTECS | XJ9095055 |
| HS Code | 2935009090 |
Customs
| HS Code | 2935009090 |
|---|---|
| Summary | 2935009090 other sulphonamides VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:6.5% General tariff:35.0% |
Articles39
More Articles| Optimization of methazolamide-loaded solid lipid nanoparticles for ophthalmic delivery using Box-Behnken design. J. Liposome Res. 24(3) , 171-81, (2014) The purpose of the present study was to optimize methazolamide (MTZ)-loaded solid lipid nanoparticles (SLNs) which were used as topical eye drops by evaluating the relationship between design factors ... | |
| Soluble CD44 and vascular endothelial growth factor levels in patients with acute primary angle closure. Acta Ophthalmol. 93 , e261-5, (2015) Acute elevation of intraocular pressure (IOP) in acute primary angle closure (APAC) can cause huge damage to the variable cells in the eye; however, the mechanisms that connect the two processes still... | |
| Meta-analysis of α2-adrenergic agonists versus carbonic anhydrase inhibitors as adjunctive therapy. Curr. Med. Res. Opin. 28(4) , 543-50, (2012) To evaluate the efficacy of α2-adrenergic agonist (AA) brimonidine and topical carbonic anhydrase inhibitors (CAIs) dorzolamide and brinzolamide in reducing intraocular pressure (IOP) when used as adj... |
Synonyms
| MFCD08067749 |
| Birnzolamide |
| Brinzolamide (BRZ) |
| 3znc |
| Azopt (TN) |
| (4R)-4-(Ethylamino)-3,4-dihydro-2-(3-methoxypropyl)-2H-thieno[3,2-e]-1,2-thiazine-6-sulfonamide 1,1-dioxide |
| (R)-(+)-4-ethylamino-2-(3-methoxypropyl)-3,4-dihydro-2H-thieno[3,2-e]-1,2-thiazine-6-sulfonamide-1,1-dioxide |
| (4R)-4-(Ethylamino)-2-(3-methoxypropyl)-3,4-dihydro-2H-thieno[3,2-e][1,2]thiazine-6-sulfonamide 1,1-dioxide |
| Azopt |
| (4R)-4-(ethylamino)-2-(3-methoxypropyl)-1,1-dioxo-3,4-dihydrothieno[3,2-e]thiazine-6-sulfonamide |
| 2H-Thieno[3,2-e]-1,2-thiazine-6-sulfonamide, 4-(ethylamino)-3,4-dihydro-2-(3-methoxypropyl)-, 1,1-dioxide, (4R)- |
| Brinzolamide [USAN] |
| Brinzolamide |
