Home Metabolism Carbonic Anhydrase inhibitor Dorzolamide HCl For research use only.

Dorzolamide HCl

Synonyms: MK-507 (L-671152) HCl

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

Dorzolamide HCl Chemical Structure

CAS No. 130693-82-2

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Dorzolamide HCl Related Products

Signaling Pathway

Carbonic Anhydrase Signaling Pathways

Carbonic Anhydrase Signaling Pathway

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
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
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]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02967614 Completed
Glaucoma|Eye Diseases|Ocular Hypertension
Kukje Pharma
 December 2016 Phase 1

Chemical Information & Solubility

Molecular Weight 360.9 Formula

C10H16N2O4S3.HCl
CAS No. 130693-82-2 SDF Download Dorzolamide HCl SDF
Smiles CCNC1CC(S(=O)(=O)C2=C1C=C(S2)S(=O)(=O)N)C.Cl
Storage (From the date of receipt)

In vitro
Batch:

Water : 37 mg/mL

DMSO : Insoluble ( Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : Insoluble


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In vivo
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