product name Dorzolamide HCl
Description: Dorzolamide HCl (also known as MK-507, or 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, it is used as anti-glaucoma agent that is topically applied in the form of eye drops. Dorzolamide hydrochloride is used to lower increased intraocular pressure in open-angle glaucoma and ocular hypertension.
References: J Ocul Pharmacol Ther. 1997 Feb;13(1):23-30; Vet Ophthalmol. 2001 Mar;4(1):61-7.
360.9
Formula
C10H16N2O4S3.HCl
CAS No.
130693-82-2
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: <1 mg/mL
Water: 14 mg/mL (38.79 mM)
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
MK-507 (L-671152) HCl
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19404537
| In Vitro |
In vitro activity: 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. Kinase Assay: Cell Assay: |
|---|---|
| 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. |
| Animal model | |
| Formulation & Dosage | |
| References | J Ocul Pharmacol Ther. 1997 Feb;13(1):23-30; Vet Ophthalmol. 2001 Mar;4(1):61-7. |
Related Posts
product name Dorzolamide HCl
Description: Dorzolamide HCl (also known as MK-507, or 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, it is used as anti-glaucoma agent that is topically applied in the form of eye drops. Dorzolamide hydrochloride is used to lower increased intraocular pressure in open-angle glaucoma and ocular hypertension.
References: J Ocul Pharmacol Ther. 1997 Feb;13(1):23-30; Vet Ophthalmol. 2001 Mar;4(1):61-7.
360.9
Formula
C10H16N2O4S3.HCl
CAS No.
130693-82-2
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: <1 mg/mL
Water: 14 mg/mL (38.79 mM)
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
MK-507 (L-671152) HCl
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19404537
| In Vitro |
In vitro activity: 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. Kinase Assay: Cell Assay: |
|---|---|
| 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. |
| Animal model | |
| Formulation & Dosage | |
| References | J Ocul Pharmacol Ther. 1997 Feb;13(1):23-30; Vet Ophthalmol. 2001 Mar;4(1):61-7. |