Brinzolamide

Modify Date: 2024-01-02 08:05:36

Brinzolamide Structure
Brinzolamide structure
 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 N/A
MSDS Chinese USA Flash Point 308.2±32.9 °C

 Use of Brinzolamide


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].

 Names

Name brinzolamide
Synonym More Synonyms

 Brinzolamide Biological Activity

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
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
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

 Synthetic Route

(S)-3,4-Dihydro-4-hydroxy-2-(3-methoxypropyl)-2H-thieno[3,2-e]-1,2-thiazine-6-sulfonamide 1,1-dioxide structure

(S)-3,4-Dihydro...

CAS#:154127-42-1
Ethylamine structure

Ethylamine

CAS#:75-04-7

~%

Brinzolamide Structure

Brinzolamide

CAS#:138890-62-7
Literature: WO2008/62463 A2, ; Page/Page column 26-27 ;
N/A structure

N/A

CAS#:1029324-92-2

~%

Brinzolamide Structure

Brinzolamide

CAS#:138890-62-7
Literature: US2010/9977 A1, ; Page/Page column 12 ;
brinzolamide maleate structure

brinzolamide maleate

CAS#:1448780-04-8

~%

Brinzolamide Structure

Brinzolamide

CAS#:138890-62-7
Literature: BIOCON LIMITED; KOTHAKONDA, Kiran Kumar; VENKATA, Srinivas Pullela; RAJMAHENDRA, Shanmughasamy; MHETRE, Sandeep Madhukar; CHANDAVARKAR, Arun Patent: WO2013/114397 A2, 2013 ; Location in patent: Page/Page column 7; 10 ;
(4R)-4-(ethylamino)-2-(3-methoxypropyl)-1,1-dioxo-3,4-dihydrothieno[3,2-e]thiazine-6-sulfonamide,hydrochloride structure

(4R)-4-(ethylam...

CAS#:150937-43-2

~%

Brinzolamide Structure

Brinzolamide

CAS#:138890-62-7
Literature: BIOCON LIMITED; KOTHAKONDA, Kiran Kumar; VENKATA, Srinivas Pullela; RAJMAHENDRA, Shanmughasamy; MHETRE, Sandeep Madhukar; CHANDAVARKAR, Arun Patent: WO2013/114397 A2, 2013 ; Location in patent: Page/Page column 7; 9 ;
Brinzolamide Impurity 2 structure

Brinzolamide Im...

CAS#:165117-54-4
Ethylamine structure

Ethylamine

CAS#:75-04-7

~48%

Brinzolamide Structure

Brinzolamide

CAS#:138890-62-7
Literature: USV LIMITED Patent: WO2008/62463 A2, 2008 ; Location in patent: Page/Page column 29-30 ;
(S)-6-Chloro-2-(3-methoxypropyl)-3,4-dihydro-2H-thieno[3,2-e][1,2]thiazin-4-ol 1,1-dioxide structure

(S)-6-Chloro-2-...

CAS#:160982-13-8

~%

Brinzolamide Structure

Brinzolamide

CAS#:138890-62-7
Literature: EP2348026 A1, ;
3-Acetyl-2,5-dichlorothiophene structure

3-Acetyl-2,5-di...

CAS#:36157-40-1

~%

Brinzolamide Structure

Brinzolamide

CAS#:138890-62-7
Literature: Organic Process Research and Development, , vol. 3, # 2 p. 114 - 120
1-(2-(benzylthio)-5-chlorothiophen-3-yl)ethanone structure

1-(2-(benzylthi...

CAS#:160982-09-2

~%

Brinzolamide Structure

Brinzolamide

CAS#:138890-62-7
Literature: Organic Process Research and Development, , vol. 3, # 2 p. 114 - 120
(S)-3,4-Dihydro-4-hydroxy-2-(3-methoxypropyl)-2H-thieno[3,2-e]-1,2-thiazine-6-sulfonamide 1,1-dioxide structure

(S)-3,4-Dihydro...

CAS#:154127-42-1

~%

Brinzolamide Structure

Brinzolamide

CAS#:138890-62-7
Literature: Organic Process Research and Development, , vol. 3, # 2 p. 114 - 120

 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

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 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
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Related Compounds: More...
Brinzolamide
138890-50-3
Brinzolamide-d5
1217651-02-9
(S)-Brinzolamide
154127-19-2
brinzolamide maleate
1448780-04-8
Brinzolamide Impurity 3
171273-35-1
Brinzolamide Impurity 5
154127-42-1
Brinzolamide Impurity 4
154127-41-0
Brinzolamide Impurity 6
160982-13-8
N-Desethyl Brinzolamide
404034-55-5
Chemsrc provides Brinzolamide(CAS#:138890-62-7) MSDS, density, melting point, boiling point, structure, formula, molecular weight etc. Articles of Brinzolamide are included as well.>> amp version: Brinzolamide

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