[CAS NO. 130693-82-2] Dorzolamide HCl

Name: Dorzolamide HCl
Brand: Arctom Scientific
SKU: SLK-S1375

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PRODUCTS SPECIFICATIONS [130693-82-2]

Store

Catalog

SLK-S1375

Brand

Selleck

CAS

130693-82-2

DESCRIPTION [130693-82-2]

Overview

MDL	MFCD00884659
Molecular Weight	360.9
Molecular Formula	C10H16N2O4S3.HCl
SMILES	O=S1(=O)C2=C([C@@H](NCC)C[C@@H]1C)C=C(S(N)(=O)=O)S2.Cl

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	2.7709 mL	13.8543 mL	27.7085 mL
5 mM	0.5542 mL	2.7709 mL	5.5417 mL
10 mM	0.2771 mL	1.3854 mL	2.7709 mL
50 mM	0.0554 mL	0.2771 mL	0.5542 mL

Description

Dorzolamide (MK-507, L-671152) HCl is a water-soluble, potent inhibitor of human and IV with 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. 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] Maren TH, et al. J Ocul Pharmacol Ther, 1997, 13(1), 23-30.
[2] Josefsson A1, et al. Exp Eye Res, 2004, 78(2), 215-221.
[3] Gelatt KN, et al. Vet Ophthalmol, 2001, 4(1), 61-67.
[4] Percicot CL, et al. J Pharmacol Toxicol Methods, 1996, 36(4), 223-228.
[5] Sugrue MF, et al. J Ocul Pharmacol Ther, 1996, 12(3), 363-376.

Synonyms

4H-Thieno[2,3-b]thiopyran-2-sulfonamide, 4-(ethylamino)-5,6-dihydro-6-methyl-, 7,7-dioxide, hydrochloride (1:1), (4S,6S)-

4H-Thieno[2,3-b]thiopyran-2-sulfonamide, 4-(ethylamino)-5,6-dihydro-6-methyl-, 7,7-dioxide, monohydrochloride, (4S-trans)-

4H-Thieno[2,3-b]thiopyran-2-sulfonamide, 4-(ethylamino)-5,6-dihydro-6-methyl-, 7,7-dioxide, monohydrochloride, (4S,6S)-

L 671152

MK 507

Trusopt

Dorzolamide hydrochloride

(S,S)-(-)-5,6-Dihydro-4-ethylamino-6-methyl-4H-thieno[2,3-b]thiopyran-2-sulfonamide-7,7-dioxide monohydrochloride

Biosopt

(4S,6S)-4-(Ethylamino)-5,6-dihydro-6-methyl-4H-thieno-[2,3-b]thiopyran-2-sulfonamide 7,7-dioxide hydrochloride