Dorzolamide HCl

Catalog No.S1375 Synonyms: MK-507 (L-671152) HCl

For research use only.

Dorzolamide (MK-507, L-671152) HCl is a water-soluble, potent inhibitor of human carbonic anhydrase II and IV with Ki of 1.9 nM and 31 nM, respectively, used as anti-glaucoma agent.

Dorzolamide HCl Chemical Structure

CAS No. 130693-82-2

Selleck's Dorzolamide HCl has been cited by 2 Publications

Purity & Quality Control

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Biological Activity

Description Dorzolamide (MK-507, L-671152) HCl is a water-soluble, potent inhibitor of human carbonic anhydrase II and IV with Ki of 1.9 nM and 31 nM, respectively, used as anti-glaucoma agent.
Targets
Carbonic anhydrase II [1] Carbonic anhydrase IV [1] Carbonic anhydrase I [1]
1.9 nM(Ki) 31 nM(Ki) 6000 nM(Ki)
In vitro

Dorzolamide is a powerful inhibitor of carbonic anhydrase (CA) II that penetrates the sclera and cornea to reach the ciliary process and lowers formation of HCO3 and aqueous humor. [1] Dorzolamide causes a vasodilatation of retinal arteries, pre-contracted by three different mechanisms by direct action and presumably independent of changes in extracellular pH. [2]

In vivo Dorzolamide, administered twice and three times daily, significantly decreases intraocular pressure (IOP) in glaucomatous dogs on the first day (twice daily 7.6 mmHg, and three times daily 16.4 mmHg) that is even greater by day 5 (twice daily 10.4 mmHg, and three times daily 13.9 mmHg). Dorzolamide (instilled in the drug eye for day 1 through to day 5) combined with oral methazolamide (administered from day 3 through to day 5) significantly lowers IOP in the eye on day 1, for day 3 and for all of day 5 for both eyes. Dorzolamide (2%) instilled three times daily produces similar IOP declines compared to the combination of oral methazolamide and 2% dorzolamide administered twice daily. [3] Dorzolamide hydrochloride induces a very large IOP reduction and is found to be also well effective at night in rabbit. [4] Dorzolamide maximally lowers the intraocular pressure (IOP) of glaucomatous monkeys by 22%, 30% and 37%, respectively. [5]

Protocol (from reference)

Solubility (25°C)

In vitro

Water 14 mg/mL
(38.79 mM)
DMSO Insoluble
Ethanol Insoluble

Chemical Information

Molecular Weight 360.9
Formula

C10H16N2O4S3.HCl

CAS No. 130693-82-2
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCNC1CC(S(=O)(=O)C2=C1C=C(S2)S(=O)(=O)N)C.Cl

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02967614 Completed Drug: [A]|Drug: [B]|Drug: [A]+[B](1)|Drug: [A]+[B](2) Glaucoma|Eye Diseases|Ocular Hypertension Kukje Pharma December 2016 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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