2. Metabolic Enzyme/Protease
  3. Carbonic Anhydrase
  4. Brinzolamide

Brinzolamide  (Synonyms: AL-4862)

Cat. No.: HY-B0588 Purity: 99.61%
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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.

For research use only. We do not sell to patients.

Brinzolamide Chemical Structure

Brinzolamide Chemical Structure

CAS No. : 138890-62-7

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 73 In-stock
Solution
10 mM * 1 mL in DMSO USD 73 In-stock
Solid
5 mg USD 42 In-stock
10 mg USD 66 In-stock
25 mg USD 132 In-stock
50 mg USD 180 In-stock
100 mg USD 252 In-stock
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Based on 3 publication(s) in Google Scholar

Other Forms of Brinzolamide:

Brinzolamide Related Antibodies

Top Publications Citing Use of Products

View All Carbonic Anhydrase Isoform Specific Products:

View All Isoforms
CA CA I CA Ⅱ CA Ⅸ CA XII

  • Biological Activity

  • Purity & Documentation

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Description

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[1][2].

IC50 & Target

CA Ⅱ

 

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
Tmax (h) 0.08 0.5 1 0.25
Cmax (ng/mL, ng/g) 11,050 1964 408 1245
Terminal t1/2 (h) 3.4 13 2 13.6
AUC0-24h (h*ng/mL, h*ng/g) 17,780 7725 1896 11414
AUC0-∞ (h*ng/mL, h*ng/g) 17,836 8839 1955 16628
Dose-normalized AUC0-∞ (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
Molecular Weight

383.51

Formula

C12H21N3O5S3
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6075 mL 13.0375 mL 26.0749 mL
5 mM 0.5215 mL 2.6075 mL 5.2150 mL
View the Complete Stock Solution Preparation Table

* 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.

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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

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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • 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.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* 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.

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
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Brinzolamide Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Brinzolamide138890-62-7AL-4862AL4862AL 4862Carbonic AnhydraseCarbonate dehydratasecarbonic anhydrase IIintraocular pressureIOPatrial fluidglaucomaInhibitorinhibitorinhibit

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