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Dorzolamide HCl Carbonic Anhydrase inhibitor

Name: Dorzolamide HCl
Brand: Selleck Chemicals
SKU: S1375
Availability: InStock
Rating: 5 (2 reviews)

Cat.No.S1375

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

Chemical Structure

Molecular Weight: 360.9

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Quality Control

Batch: Purity: 99.96%

99.96

Related Targets	Dehydrogenase HSP Transferase P450 (e.g. CYP17) PDE phosphatase PPAR Vitamin Carbohydrate Metabolism Mitochondrial Metabolism
Other Carbonic Anhydrase Inhibitors	U-104 (SLC-0111) Indisulam (E7070) Benzenesulfonamide Tioxolone 2-Aminobenzenesulfonamide

Solubility

In vitro
Batch:

Water : 37 mg/mL

DMSO : Insoluble
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

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% DMSO

% Tween 80

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

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

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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Chemical Information, Storage & Stability

Molecular Weight	360.9	Formula	C₁₀H₁₆N₂O₄S₃.HCl	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	130693-82-2	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	MK-507 (L-671152) HCl			Smiles	CCNC1CC(S(=O)(=O)C2=C1C=C(S2)S(=O)(=O)N)C.Cl

Mechanism of Action

Targets/IC₅₀/Ki	Carbonic anhydrase II 1.9 nM(Ki) Carbonic anhydrase IV 31 nM(Ki) Carbonic anhydrase I 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. Dorzolamide causes a vasodilatation of retinal arteries, pre-contracted by three different mechanisms by direct action and presumably independent of changes in extracellular pH.
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. Dorzolamide hydrochloride induces a very large IOP reduction and is found to be also well effective at night in rabbit. Dorzolamide maximally lowers the intraocular pressure (IOP) of glaucomatous monkeys by 22%, 30% and 37%, respectively.
References	[1] https://pubmed.ncbi.nlm.nih.gov/9029437/ [2] https://pubmed.ncbi.nlm.nih.gov/14729354/ [3] https://pubmed.ncbi.nlm.nih.gov/11397321/ [4] https://pubmed.ncbi.nlm.nih.gov/9040114/ [5] https://pubmed.ncbi.nlm.nih.gov/8875343/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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