For research use only.
Catalog No.S1375 Synonyms: MK-507 (L-671152) HCl
CAS No. 130693-82-2
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.
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|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.|
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. |
-  Maren TH, et al. J Ocul Pharmacol Ther, 1997, 13(1), 23-30.
-  Josefsson A1, et al. Exp Eye Res, 2004, 78(2), 215-221.
-  Gelatt KN, et al. Vet Ophthalmol, 2001, 4(1), 61-67.
|In vitro||Water||14 mg/mL (38.79 mM)|
* 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.
|Synonyms||MK-507 (L-671152) HCl|
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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|
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