Dorzolamide HCl

Catalog No.S1375 Batch:S137501

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Technical Data

Formula

C10H16N2O4S3.HCl

Molecular Weight 360.9 CAS No. 130693-82-2
Solubility (25°C)* In vitro Water 14 mg/mL (38.79 mM)
DMSO Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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)

Selleck's Dorzolamide HCl has been cited by 2 publications

The comparative integrated multi-omics analysis identifies CA2 as a novel target for chordoma [ Neuro Oncol, 2021, noab156] PubMed: 34214167
A Comparative Study of Drug Affinities Determined by Thermofluor and Kinetic Analysis [ ETD, 2020, N/A] PubMed: N/A

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.