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

Brinzolamide  (Synonyms: AL-4862)

Cat. No.: HY-B0588 Purity: 99.33%
COA Handling Instructions

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

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10 mM * 1 mL in DMSO USD 73 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
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ready for reconstitution
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Solid
10 mg USD 66 In-stock
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50 mg USD 198 In-stock
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100 mg USD 290 In-stock
Estimated Time of Arrival: December 31
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Based on 3 publication(s) in Google Scholar

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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

IC50: 3.2 nM (carbonic anhydrase II) [2].

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

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.
SMILES

O=S(C(S1)=CC2=C1S(N(CCCOC)C[[email protected]@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 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (260.75 mM; Need ultrasonic)

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
10 mM 0.2607 mL 1.3037 mL 2.6075 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are available by MCE.
Purity & Documentation
References
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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.

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Brinzolamide
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