ChemicalBook > CAS DataBase List > Brinzolamide

Brinzolamide

Product Name
Brinzolamide
CAS No.
138890-62-7
Chemical Name
Brinzolamide
Synonyms
Azopt;AL 4;CT4.7;GAGE7;GAGE-7;GAGE-8;CS-138;GAGE-7B;AL 4862;AL-4682
CBNumber
CB3458912
Molecular Formula
C12H21N3O5S3
Formula Weight
383.51
MOL File
138890-62-7.mol
More
Less

Brinzolamide Property

Melting point:
130.0 to 134.0 °C
Boiling point:
586.0±60.0 °C(Predicted)
Density 
1.50±0.1 g/cm3(Predicted)
storage temp. 
-20°C
solubility 
DMSO: ≥10mg/mL
form 
powder
pka
9.62±0.40(Predicted)
color 
white to beige
Merck 
14,1376
InChIKey
HCRKCZRJWPKOAR-JTQLQIEISA-N
CAS DataBase Reference
138890-62-7(CAS DataBase Reference)
More
Less

Safety

WGK Germany 
3
RTECS 
XJ9095055
HS Code 
2935904000
More
Less

Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P501Dispose of contents/container to..…

More
Less

N-Bromosuccinimide Price

Sigma-Aldrich
Product number
SML0216
Product name
Brinzolamide
Purity
≥98% (HPLC)
Packaging
10mg
Price
$129
Updated
2024/03/01
Sigma-Aldrich
Product number
1076363
Product name
Brinzolamide
Purity
United States Pharmacopeia (USP) Reference Standard
Packaging
200mg
Price
$436
Updated
2024/03/01
TCI Chemical
Product number
B4258
Product name
Brinzolamide
Purity
>98.0%(HPLC)
Packaging
25mg
Price
$69
Updated
2024/03/01
TCI Chemical
Product number
B4258
Product name
Brinzolamide
Purity
>98.0%(HPLC)
Packaging
100mg
Price
$197
Updated
2024/03/01
Cayman Chemical
Product number
11660
Product name
Brinzolamide
Purity
≥98%
Packaging
10mg
Price
$33
Updated
2024/03/01
More
Less

Brinzolamide Chemical Properties,Usage,Production

Description

Brinzolamide is a carbonic anhydrase inhibitor developed by Alcon (now Novartis) as a treatment for primary and open-angle glaucoma and ocular hypertension. It was First approval in the United States in 1998 under the trade name Azopt. It is the second of this class after dorzolamide (1995). Brinzolamide was approved as a generic medication in the United States in November 2020.Brinzolamide is a white powder commercially formulated as a 1% ophthalmic suspension to reduce intraocular pressure (IOP). In patients with primary open-angle glaucoma or ocular hypertension, brinzolamide produced significant reductions in IOP and showed less ocular discomfort than dorzolamide.

Chemical Properties

Brinzolamide has a molecular weight of 383.5 and a melting point of about 131°C. It is a white powder or crystalline Solid, which is insoluble in water, very soluble in methanol and soluble in ethanol.

Originator

Alcon (US)

Uses

Brinzolamide is a sulfonamide and carbonic anhydrase inhibitor with specific affinity for carbonic anhydrase II. Following topical ocular administration, brinzolamide inhibits carbonic anhydrase II, an enzyme that is responsible for the movement of sodium and fluid transport in the eye. This inhibition leads to a decrease in aqueous humor secretion, probably by slowing the formation of bicarbonate ions, and results in a reduction in intraocular pressure. Brinzolamide is used to treat increased pressure in the eye caused by open-angle glaucoma.

Uses

Brinzolamide has been used as a melanin binding compound or drug in melanin binding assays. It has also been used as a carbonic anhydrase inhibitor (CAI).

Definition

ChEBI: Brinzolamide is a sulfonamide and a thienothiazine. It has a role as an antiglaucoma drug and an EC 4.2.1.1 (carbonic anhydrase) inhibitor.

Preparation

Brinzolamide synthesis method: using thiophene as raw material, 3-acetyl-2,5-dichlorothiophene (4) is obtained by chlorination and acetylation, and 4 is reacted with sodium benzyl sulfide to obtain 6,6, which is chlorinated and ammoniated. Chemical and oxidation reactions "one-pot" synthesis of 7, Carbon-based α-hydrobromination of 7 with Pyridinium tribromide gives 9,9 is asymmetrically reduced under the action of (+)-Ipc2BCl to obtain 11, which is then subjected to N-alkylation and sulfonamidation to generate (S)-3,4-dihydro-4-hydroxy-2-(3-methoxyl propyl)-2H-thieno[3,2-e]-1,2-thiazine-6-sulfonamide-1,1-dioxide, the sulfonamide group was protected with trimethyl orthoacetate to give 15 , first introduce p-toluenesulfonyl group and then replace it with ethylamino group, and remove the sulfonamide group protecting group to obtain brinzolamide. The synthesis of intermediate 4 in this route is convenient, and each step of the reaction does not require column chromatography, and the total yield is 13.4%.
Graphical Synthetic Routes of Olanzapine

Indications

Brinzolamide, a heterocyclic sulfonamide, is a topical CAI suspension that has a high affinity for the carbonic anhydrase II isoenzyme.Because the ocular hypotensive effect of the drug is equivalent whether dosed twice or three times daily, brinzolamide 1% may be administered twice daily.

brand name

Azopt (Alcon).

Therapeutic Function

Antiglaucoma

General Description

Brinzolamide is a small molecular weight compound that has an ability to bind melanin. This drug is used in ocular therapy.

Biochem/physiol Actions

Brinzolamide is a carbonic anhydrase II inhibitor used to lower intraocular pressure.

Clinical Use

Brinzolamide is indicated for the treatment of elevated IOP in patients with ocular hypertension or open-angle glaucoma.The drug is commercially available as a sterile 1.0% aqueous suspension with a pH of approximately 7.5. BAC 0.01% is added as a preservative.
The efficacy and safety of brinzolamide 1%, either two or three times daily, were evaluated in 572 patients with open-angle glaucoma or ocular hypertension against timolol 0.5% twice daily and dorzolamide 2.0% three times daily. Mean IOP changes were -3.8 to -5.7 mm Hg, -4.2 to -5.6 mm Hg, and-4.3 to-5.9 mm Hg for two- and three-times-daily brinzolamide and dorzolamide dosing, respectively. The mean IOP changes for timolol 0.5% ranged from -5.6 to -6.3 mm Hg (Figure 10-15). Brinzolamide was well tolerated, with 1.8% (twice daily) and 3% (three times daily) of patients reporting ocular discomfort versus 16.4% with dorzolamide. Complaints of blurred vision were higher with brinzolamide (5–6%) than dorzolamide (1%) or timolol (0%).
A meta-analysis of randomized clinical trials reported peak ocular hypotensive effect on IOP of 17% (19% to 15%) and trough effect of 17% (19% to 15%).

Side effects

Both brinzolamide and dorzolamide exhibit similar taste abnormalities. A single case report of the development of metabolic acidosis from topical brinzolamide has been described after twice-daily dosing. Other adverse events are negligible for brinzolamide except for some blurring of vision, attributable to its suspension vehicle.

Veterinary Drugs and Treatments

Brinzolamide is chemically similar to dorzolamide and reduces aqueous humor production by altering H+/Na+ active transport mechanisms associated with aqueous humor production in the ciliary epithelial cells. It can be used as a substitute for dorzolamide and some patients that exhibit excessive topical irritation following application of dorzolamide drops, tolerate brinzolamide better or vice versa. Cats seem to be particularly sensitive to irritation from topical dorzolamide and often brinzolamide can be used in these patients. Comparative data is available suggesting that brinzolamide and dorzolamide are equally effective in animal patients.

Precautions

Brinzolamide has the same contraindications and precautions as dorzolamide.

References

[1] desantis l. preclinical overview of brinzolamide. surv ophthalmol. 2000 jan;44 suppl 2:s119-29.

Brinzolamide Preparation Products And Raw materials

Raw materials

Sodium hypochlorite Benzyl chloride tert-Butyl methyl ether 2,5-Dichlorothiophene Chlorine Sulfurous Acid Ethyl acetate Sodium tungstate dihydrate

Preparation Products

More
Less

Brinzolamide Suppliers

Americas 1 Brazil 1 Canada 4 China 292 Europe 3 France 4 Germany 4 Greece 1 India 73 Italy 3 Japan 1 Malaysia 1 Mexico 1 Poland 1 South Korea 2 Spain 2 Switzerland 1 The Netherlands 1 United Arab Emirates 1 United Kingdom 12 United States 37 Global 446
Jai Radhe Sales
Tel
+(91)-(79)-26431096/65255722
Fax
+(91)-(79)-26569884
Email
info@jairadhesales.com
Country
India
ProdList
397
Advantage
60
TCI Chemicals (India) Pvt. Ltd.
Tel
--
Fax
--
Email
sales-in@tcichemicals.com
Country
India
ProdList
6768
Advantage
58
Manus Aktteva
Tel
--
Fax
--
Email
info@manusaktteva.in
Country
India
ProdList
581
Advantage
34
Jigs Chemical Limited
Tel
--
Fax
--
Email
info@jigschemical.com
Country
India
ProdList
235
Advantage
58
Oceanic Pharmachem Pvt. Ltd.
Tel
--
Fax
--
Email
info@oceanicpharmachem.com
Country
India
ProdList
2005
Advantage
58
Indoco Remedies Ltd.
Tel
--
Fax
--
Email
corpcom@indoco.com
Country
India
ProdList
16
Advantage
58
Pharma Affiliates
Tel
--
Fax
--
Email
@pharmaffiliates.com
Country
India
ProdList
6754
Advantage
58
ChemiSyn
Tel
--
Fax
--
Email
info@chemisyn.com
Country
India
ProdList
15
Advantage
58
BIOCON LIMITED
Tel
--
Fax
--
Email
info@biocon.com
Country
India
ProdList
12
Advantage
58
Hetero Drugs Limited
Tel
--
Fax
--
Country
India
ProdList
174
Advantage
58
Ayon PharmaChem
Tel
--
Fax
--
Email
bhargav@ayonpharmachem.com
Country
India
ProdList
303
Advantage
58
Aster International Pharmaceuticals LLP
Tel
--
Fax
--
Email
info@asterintl.com
Country
India
ProdList
113
Advantage
58
Placid Pharmachem
Tel
--
Fax
--
Email
parikshitjain@vsnl.com
Country
India
ProdList
115
Advantage
58
Samex Overseas
Tel
--
Fax
--
Country
India
ProdList
124
Advantage
58
BDR Pharmaceuticals International Pvt., Ltd.
Tel
--
Fax
--
Email
marketing@bdrpharma.com
Country
India
ProdList
91
Advantage
58
International Drug & Chemical Co.
Tel
--
Fax
--
Email
sales@idcco.com
Country
India
ProdList
65
Advantage
58
Ralington Pharma.
Tel
--
Fax
--
Email
info@ralingtonpharma.com
Country
India
ProdList
311
Advantage
58
Rely Chem
Tel
--
Fax
--
Country
India
ProdList
125
Advantage
58
USV PRIVATE LIMITED
Tel
--
Fax
--
Email
info@usv.in
Country
India
ProdList
22
Advantage
58
Bakul Pharma Private Limited
Tel
--
Fax
--
Country
India
ProdList
37
Advantage
58
Pharvinex Life Science LLP
Tel
--
Fax
--
Email
info@pharvinex.com
Country
India
ProdList
55
Advantage
58
Clearsynth Labs
Tel
--
Fax
--
Email
fo@clearsynth.com
Country
India
ProdList
3887
Advantage
58
Aspen Biopharma Labs Pvt Ltd
Tel
--
Fax
--
Email
info@aspenbiopharmalabs.com
Country
India
ProdList
52
Advantage
58
Sai Prathyu Marketing
Tel
--
Fax
--
Country
India
ProdList
162
Advantage
58
Trichem Healthcare Pvt. Ltd.
Tel
--
Fax
--
Email
info@tricheminc.net
Country
India
ProdList
9
Advantage
58
Nivi Exim
Tel
--
Fax
--
Email
info@niviexim.com
Country
India
ProdList
61
Advantage
58
Flax Laboratories
Tel
--
Fax
--
Email
info@flaxlaboratories.com
Country
India
ProdList
13
Advantage
58
CTX Lifesciences Private Limited
Tel
--
Fax
--
Country
India
ProdList
9
Advantage
58
Globofarm International Private Limited
Tel
--
Fax
--
Email
procurement@globofarm.net
Country
India
ProdList
188
Advantage
58
Biocon India Pvt Ltd
Tel
--
Fax
--
Email
contact.us@biocon.com
Country
India
ProdList
18
Advantage
58
BDR Pharmaceuticals International Pvt. Ltd
Tel
--
Fax
--
Country
India
ProdList
23
Advantage
58
Olympus Chemicals & Fertilizers
Tel
--
Fax
--
Country
India
ProdList
486
Advantage
58
JD Chem India
Tel
--
Fax
--
Email
sales@jdchecm.co.in
Country
India
ProdList
38
Advantage
58
Century Pharmaceuticals Limited
Tel
--
Fax
--
Country
India
ProdList
22
Advantage
58
Eastern Chemicals (Mumbai) Pvt., Ltd.
Tel
--
Fax
--
Email
info@ecmpl.com
Country
India
ProdList
104
Advantage
58
Disha APIs Pvt Ltd
Tel
--
Fax
--
Email
info@dishaapis.com
Country
India
ProdList
90
Advantage
58
Athos Chemicals
Tel
--
Fax
--
Email
export@athoschemicals.com
Country
India
ProdList
315
Advantage
58
Niksan Pharmaceutical
Tel
--
Fax
--
Email
niksanpharmaceutical@yahoo.com
Country
India
ProdList
18
Advantage
58
Jai Radhe Sales
Tel
--
Fax
--
Email
nikunj@jairadhesales.com
Country
India
ProdList
157
Advantage
57
Aarti Healthcare Limited
Tel
--
Fax
--
Country
India
ProdList
28
Advantage
58
CENTURY PHARMACEUTICALS LTD
Tel
--
Fax
--
Email
info@centurypharma.com
Country
India
ProdList
21
Advantage
58
Vcare Medicines
Tel
--
Fax
--
Country
India
ProdList
114
Advantage
58
Seema Biotech
Tel
--
Fax
--
Country
India
ProdList
32
Advantage
58
INDOCO REMEDIES LIMITED
Tel
--
Fax
--
Email
abhilash.soral@indoco.com
Country
India
ProdList
18
Advantage
58
Mahalaxmi Chemi Pharma
Tel
--
Fax
--
Country
India
ProdList
11
Advantage
58
Alcove International
Tel
--
Fax
--
Country
India
ProdList
12
Advantage
58
Pharmaffiliates Analytics and Synthetics P. Ltd
Tel
--
Fax
--
Email
mktg@pharmaffiliates.com
Country
India
ProdList
6739
Advantage
58
SynZeal Research Pvt Ltd
Tel
--
Fax
--
Email
standards@synzeal.com
Country
India
ProdList
6514
Advantage
58
A.J Chemicals
Tel
--
Fax
--
Email
sales@ajchem.in
Country
India
ProdList
6100
Advantage
58
BIOCON LTD
Tel
--
Fax
--
Email
info@biocon.com
Country
India
ProdList
39
Advantage
58
More
Less

View Lastest Price from Brinzolamide manufacturers

WUHAN FORTUNA CHEMICAL CO., LTD
Product
Brinzolamide 138890-62-7
Price
US $1.00/g
Min. Order
1g
Purity
98.0%~102.0%,USP41
Supply Ability
20kg/month
Release date
2021-06-04
Apeloa production Co.,Limited
Product
Brinzolamide 138890-62-7
Price
US $1.00/g
Min. Order
1g
Purity
0.98
Supply Ability
1000
Release date
2024-07-19
shandong perfect biotechnology co.ltd
Product
Brinzolamide 138890-62-7
Price
US $0.00/g
Min. Order
1g
Purity
98% HPLC
Supply Ability
1kg
Release date
2023-08-03

138890-62-7, BrinzolamideRelated Search:

Brinzolamide-d5 3,4-Dihydro-2-(3-methoxypropyl)-4-oxo-2H-thieno[3,2-e]-1,2-thiazine-6-sulfonamide 1,1-dioxide BrinzolaMide IMpurity C Tafluprost Bendazac L-lysine Pirenoxine Fluorometholone Pranoprofen Itraconazole Brimonidine 3,4'-Dihexyl-2,2'-bithiophene Carbonic Anhydrase IX/XII Inhibitor II(U-104) ENALAPRILAT DIHYDRATE Fosinopril sodium Dexmedetomidine Belinostat (PXD101) Entinostat rac Brinzolamide-d5

  • H-Thieno[3,2-e]-1,2-thiazine-6-sulfonamide, 4-(ethylamino)-3,4-dihydro-2-(3-methoxypropyl)-, 1,1-dioxide, (4R)-
  • Brinzolamide (R)-4-(Ethylamino)-3,4-dihydro-2-(3-methoxypropyl)-2H-thieno[3,2-e]-1,2-thiazine-6-sulfonamide 1,1-dioxide
  • (5R)-5-Ethylamino-3-(3-methoxypropyl)-2,2-dioxo-2?6,9-dithia-3-azabicyclo[4.3.0]nona-7,10-diene-8-sulfonamide
  • ANTI-GAGE7 (C-TERM) antibody produced in rabbit
  • Cancer/testis antigen 4.7
  • CT4.7
  • G antigen 7
  • GAGE-12I
  • GAGE7
  • GAGE-7
  • GAGE-7B
  • GAGE-8
  • Brinzolamide, >=98%
  • BIRNZOLAMIDE
  • BRINZOLAMIDE
  • (4R)-4-(Ethylamino)-3,4-dihydro-2-(3-methoxypropyl)-2H-thieno[3,2-e]-1,2-thiazine-6-sulfonamid
  • 2H-Thieno[3,2-e]-1,2-thiazine-6-sulfonamide, 4-(ethylamino)-3,4-dihydro-2-(3-methoxypropyl)-, 1,1-dioxide, (4R)-
  • 2H-Thieno[3,2-e]-1,2-thiazine-6-sulfonamide, 4-(ethylamino)-3,4-dihydro-2-(3-methoxypropyl)-, 1,1-dioxide, (R)-
  • CS-138
  • BIRNZOLAMIDE BRINZOLAMIDE 2H-Thieno[3,2-e]-1,2-thiazine-6-sulfonamide, 4-(ethylamino)-3,4-dihydro-2-(3-methoxypropyl)-, 1,1-dioxide, (R)- AL 4862 Brinlolamide (4R)-4-(Ethylamino)-3,4-dihydro-2-(3-methoxypropyl)-2H-thieno[3,2-e]-1,2-thiazine-6-sulfonamide
  • Brinzolamide-017-R
  • AL 4862
  • Brinlolamide
  • (R)-4-(Ethylamino)-3,4-dihydro-2-(3-methoxypropyl)-2H-thieno[3,2-e]-1,2-thiazine-6-sulfonamide 1,1-dioxide
  • (4R)-4-(Ethylamino)-3,4-dihydro-2-(3-methoxypropyl)-2H-thieno[3,2-e]-1,2-thiazine-6-sulfonamide 1,1-Dioxide
  • AL-4682
  • Azopt
  • -4-(Ethylamino)-3，4-dihydro-2-(3-methoxypropyl)-2H-thieno[3，2-e]-1，2-thiazine-6-sulfonamide1，1-dioxide
  • (4R)-4-(ethylamino)-1,1-diketo-2-(3-methoxypropyl)-3,4-dihydrothieno[3,2-e]thiazine-6-sulfonamide
  • (4R)-4-(ethylamino)-2-(3-methoxypropyl)-1,1-dioxo-3,4-dihydrothieno[3,2-e][1,2]thiazine-6-sulfonamide
  • (4R)-4-(ethylamino)-2-(3-methoxypropyl)-1,1-dioxo-3,4-dihydrothieno[3,2-e]thiazine-6-sulfonamide
  • Brinzolamide (200 mg)
  • AL 4
  • (4R)-4-(ethylaMino)-2-(3-Methoxypropyl)-1,1-dioxo-2H,3H,4H-1$l^{6},7,2-thieno[3,2-e][1$l^{6},2]thiazine-6-sulfonaMide
  • Brinzolamide &gt
  • (R)-4-(Ethylamino)-2-(3-methoxypropyl)-3,4-dihydro-2H-thieno[3,2-e][1,2]thiazine-6-sulfonamide 1,1-dioxide
  • Bromobenzoamide
  • Brinzolamide USP/EP/BP
  • BrinzolamideQ: What is Brinzolamide Q: What is the CAS Number of Brinzolamide Q: What is the storage condition of Brinzolamide Q: What are the applications of Brinzolamide
  • Brinzolamide (1076363)
  • 138890-62-7
  • 38890-62-7
  • C12H21N3O5S3
  • BETOPTIC
  • Chiral Reagents
  • Intermediates & Fine Chemicals
  • Pharmaceuticals
  • Brinzolamide
  • 138890-62-7