Dorzolamide HCl

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

Dorzolamide HCl Chemical Structure

Molecular Weight(MW): 360.9

Dorzolamide 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.

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Biological Activity

Description Dorzolamide 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

Solubility (25°C)

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

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 360.9
Formula

C10H16N2O4S3.HCl

CAS No. 130693-82-2
Storage powder
in solvent
Synonyms MK-507 (L-671152) HCl

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02852057 Recruiting Glaucoma University of Florida January 18 2018 Phase 1
NCT02852057 Recruiting Glaucoma University of Florida January 18 2018 Phase 1
NCT03193333 Recruiting Primary Open-angle Glaucoma Laboratorios Sophia S.A de C.V. August 4 2017 Phase 3
NCT03193333 Recruiting Primary Open-angle Glaucoma Laboratorios Sophia S.A de C.V. August 4 2017 Phase 3
NCT03034772 Recruiting Neovascular Age-related Macular Degeneration|Wet Macular Degeneration Wills Eye|Mid Atlantic Retina February 8 2017 Phase 2|Phase 3
NCT03034772 Recruiting Neovascular Age-related Macular Degeneration|Wet Macular Degeneration Wills Eye|Mid Atlantic Retina February 8 2017 Phase 2|Phase 3

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Carbonic Anhydrase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID