Art. -Nr.: HY-B0588

Brinzolamide

(Synonyms: AL-4862)

7 Cited Publications

Kundenbewertung

Based on 7 publication(s) in Google Scholar

Brinzolamide (AL-4862) is a selective carbonic anhydrase II inhibitor with anIC₅₀ value of 3.2 nM. Brinzolamide hydrochloride reduces intraocular pressure (IOP) by inhibiting ciliary CA-II and decreasing atrial fluid secretion. Brinzolamide can be used in glaucoma disease research.

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Reinheit: 99.91%
CAS. Nr.: 138890-62-7
Formel: C₁₂H₂₁N₃O₅S₃
Molecular Weight:383.51

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Brinzolamide Chemical Structure

CAS. Nr.: 138890-62-7

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vivo
- Clinical Trial
Chemical Information
Publications (7)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

CA Ⅱ

Alle Carbonic Anhydrase Isoform-spezifische Produkte anzeigen :

In Vivo

Brinzolamide (7.5 mg or 12 mg) implanted in a silicone matrix is extremely well tolerated and provides sustained release of brinzolamide and significant reduction in intraocular pressure (IOP) for up to 28 days with no adverse effects or signs of toxicity in normotensive NZW rabbits^[2].
The pharmacokinetic parameters of Brinzolamide in rabbits^[1].

	Intracameral Administration (4.5 mg)	Intracameral Administration (4.5 mg)	Topical Administration (500 mg)	Topical Administration (500 mg)
PK Parameters	Aqueous Humor	Iris-Ciliary Body	Aqueous Humor	Iris-Ciliary Body
T_max (h)	0.08	0.5	1	0.25
C_max (ng/mL, ng/g)	11,050	1964	408	1245
Terminal t_1/2 (h)	3.4	13	2	13.6
AUC_{0-24h (hng/mL, hng/g)}	17,780	7725	1896	11414
AUC_0-∞ (hng/mL, hng/g)	17,836	8839	1955	16628
Dose-normalized AUC_0-∞ (h/mL, h/g)	4	2	0.004	0.03

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Rabbits^[2]
Dosage:

7.5 mg, 12 mg
Administration:

Brinzolamide silicone matrix implant placed in the episcleral space
Result:

Resulted in a significant IOP reduction of 4.6 mmHg on days 10-28, with concentrations of 12 mg.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 138890-62-7
Appearance Solid
Molecular Weight 383.51
Formel C₁₂H₂₁N₃O₅S₃
Color Light yellow to yellow
SMILES

O=S(C(S1)=CC2=C1S(N(CCCOC)C[C@@H]2NCC)(=O)=O)(N)=O
Synonyms

AL-4862
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (7)

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Mater Today Bio

Brinzolamide encapsulated β-cyclodextrin-chondroitin sulfate nanocomplexes anchored chitosan/polycaprolactone nanofibers as an ocular insert for glaucoma treatment. [Abstract]

2025 Aug 11:34:102179. PMID: 40838214
ACS Environ Au

Machine Learning-Assisted Recognition of Environmental Sulfur-Containing Chemicals in Nontargeted Mass Spectrometry Analysis of Inadequate Mass Resolution. [Abstract]

2025 Aug 5;5(6):573-582. PMID: 41277996
Anal Chem

Exposome-Scale Investigation of Cl-/Br-Containing Chemicals Using High-Resolution Mass Spectrometry, Multistage Machine Learning, and Cloud Computing. [Abstract]

2025 Jun 3;97(21):11099-11109. PMID: 40401576
Anal Chem

Comparability of Raman Spectroscopic Configurations: A Large Scale Cross-Laboratory Study. [Abstract]

2020 Dec 15;92(24):15745-15756. PMID: 33225709
J Pharm Biomed Anal

Screening method of mildronate and over 300 doping agents by reversed-phase liquid chromatography-high resolution mass spectrometry. [Abstract]

2021 Feb 20:195:113870. PMID: 33453569
J Pharm Innov

2025 Oct 14;20(5):1-22.
ETH Zurich

2020 Dec.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (260.75 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.6075 mL

13.0375 mL

26.0749 mL

5 mM

0.5215 mL

2.6075 mL

5.2150 mL

10 mM

0.2607 mL

1.3037 mL

2.6075 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.75 mg/mL (7.17 mM); Clear solution

This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.75 mg/mL (7.17 mM); Clear solution

This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.75 mg/mL (7.17 mM); Clear solution

This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Vatsala Naageshwaran, et al. Comprehensive Ocular and Systemic Pharmacokinetics of Brinzolamide in Rabbits After Intracameral, Topical, and Intravenous Administration. J Pharm Sci. 2021 Jan;110(1):529-535. [Content Brief]

[2]. Sara M.Smith, et al. Tolerability, pharmacokinetics, and pharmacodynamics of a brinzolamide episcleral sustained release implant in normotensive New Zealand white rabbits,Journal of Drug Delivery Science and Technology,Volume 61,2021,102123,ISSN 1773-2247

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.6075 mL	13.0375 mL	26.0749 mL	65.1873 mL
	5 mM	0.5215 mL	2.6075 mL	5.2150 mL	13.0375 mL
	10 mM	0.2607 mL	1.3037 mL	2.6075 mL	6.5187 mL
	15 mM	0.1738 mL	0.8692 mL	1.7383 mL	4.3458 mL
	20 mM	0.1304 mL	0.6519 mL	1.3037 mL	3.2594 mL
	25 mM	0.1043 mL	0.5215 mL	1.0430 mL	2.6075 mL
	30 mM	0.0869 mL	0.4346 mL	0.8692 mL	2.1729 mL
	40 mM	0.0652 mL	0.3259 mL	0.6519 mL	1.6297 mL
	50 mM	0.0521 mL	0.2607 mL	0.5215 mL	1.3037 mL
	60 mM	0.0435 mL	0.2173 mL	0.4346 mL	1.0865 mL
	80 mM	0.0326 mL	0.1630 mL	0.3259 mL	0.8148 mL
	100 mM	0.0261 mL	0.1304 mL	0.2607 mL	0.6519 mL

Keywords

Brinzolamide

7 Cited Publications

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Brinzolamide

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Publications Citing Use of MedChemExpress (MCE) Brinzolamide

Alle Carbonic Anhydrase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (7)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Brinzolamide

Metabolism/Protease Compound Library

FDA-Approved Drug Library

Drug Repurposing Compound Library

Anti-Cardiovascular Disease Compound Library

Anti-COVID-19 Compound Library

FDA Approved & Pharmacopeial Drug Library

Targeted Diversity Library

EMA-Approved Drug Library

Human Metabolite Library

Heterocyclic Compound Library

Off-patent Drug Library

Metabolic Enzyme Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Publications Citing Use of MedChemExpress (MCE) Brinzolamide

Alle Carbonic Anhydrase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (7)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Brinzolamide Related Classifications

HY-B0588 Related Classifications