Dorzolamide HCl

Carbonic anhydrase inhibitor CAS# 130693-82-2

Dorzolamide HCl

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Dorzolamide HCl

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Chemical Properties of Dorzolamide HCl

Cas No. 130693-82-2 SDF Download SDF
PubChem ID 6918132 Appearance Powder
Formula C10H17ClN2O4S3 M.Wt 360.9
Type of Compound N/A Storage Desiccate at -20°C
Synonyms L671152 hydrochloride; MK507 hydrochloride
Solubility DMSO : 100 mg/mL (277.09 mM; Need ultrasonic)
H2O : 12.5 mg/mL (34.64 mM; Need ultrasonic)
Chemical Name (4S,6S)-4-(ethylamino)-6-methyl-7,7-dioxo-5,6-dihydro-4H-thieno[2,3-b]thiopyran-2-sulfonamide;hydrochloride
SMILES CCNC1CC(S(=O)(=O)C2=C1C=C(S2)S(=O)(=O)N)C.Cl
Standard InChIKey OSRUSFPMRGDLAG-QMGYSKNISA-N
Standard InChI InChI=1S/C10H16N2O4S3.ClH/c1-3-12-8-4-6(2)18(13,14)10-7(8)5-9(17-10)19(11,15)16;/h5-6,8,12H,3-4H2,1-2H3,(H2,11,15,16);1H/t6-,8-;/m0./s1
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Dorzolamide HCl

DescriptionDorzolamide Hcl(L671152 Hcl; MK507 Hcl) is an anti-glaucoma agent, which is a carbonic anhydrase inhibitor. Target: carbonic anhydrase (CA) Dorzolamide hydrochloride is a carbonic anhydrase inhibitor. It is an anti-glaucoma agent, and acts by decreasing the production of aqueous humour [1]. Glaucoma was induced in the right eye of adult Wistar rats by episcleral venous occlusion. One experimental group was administered dorzolamide hydrochloride 2%-timolol 0.5% combination eye drops, while the other experimental group was administered dorzolamide hydrochloride2% eye drops. Control groups had surgery without drug administration. Drug application was initiated either 2 weeks before surgery (Group A), from the day of surgery (Group B), 2 weeks after surgery (Group C), or 4 weeks after surgery (Group D). RGCs were labeled by intratectal Fluorogold injections and counted from flat-mount preparations, and IOP was measured using Tonopen. Both dorzolamide-timolol combination and dorzolamide hydrochloride, when applied topically, significantly reduced IOP and improved RGC densities in experimental eyes when compared to control eyes. Earlier initiation, as well as longer duration of drug application, resulted in higher RGC densities [2]. Clinical indications: Glaucoma; Ocular hypertension FDA Approved Date: 1995 Toxicity: Dizziness, headache, shortness of breath, slow heartbeat, severe asthma, cardiac arrest

References:
[1]. Rankin AJ, et al. Effects of ocular administration of ophthalmic 2% dorzolamide hydrochloride solution on aqueous humor flow rate and intraocular pressure in clinically normal cats. Am J Vet Res. 2012 Jul;73(7):1074-8. [2]. Sarup V, et al. Dorzolamide and timolol saves retinal ganglion cells in glaucomatous adult rats. J Ocul Pharmacol Ther. 2005 Dec;21(6):454-62.

Dorzolamide HCl Dilution Calculator

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Dorzolamide HCl Molarity Calculator

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Preparing Stock Solutions of Dorzolamide HCl

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.7709 mL 13.8543 mL 27.7085 mL 55.417 mL 69.2713 mL
5 mM 0.5542 mL 2.7709 mL 5.5417 mL 11.0834 mL 13.8543 mL
10 mM 0.2771 mL 1.3854 mL 2.7709 mL 5.5417 mL 6.9271 mL
50 mM 0.0554 mL 0.2771 mL 0.5542 mL 1.1083 mL 1.3854 mL
100 mM 0.0277 mL 0.1385 mL 0.2771 mL 0.5542 mL 0.6927 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on Dorzolamide HCl

Dorzolamide HCl is a carbonic anhydrase inhibitor.

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References on Dorzolamide HCl

Simultaneous determination of dorzolamide HCL and timolol maleate in eye drops by two different spectroscopic methods.[Pubmed:11929684]

J Pharm Biomed Anal. 2002 Apr 15;28(2):391-7.

Two-component mixtures of dorzolamide hydrochloride and timolol maleate were assayed by first derivative and ratio derivative spectrophotometric methods. The first method, derivative spectrophotometry, by the zero-crossing measurements, was used due to the drugs closely overlapping absorption spectra. Linear calibration graphs of first derivative values at 250.3 nm for dorzolamide hydrochloride and 315.8 nm for timolol maleate. The second method, is based on ratio first derivative spectrophotometry, the amplitudes in the first derivative of the ratio spectra at 242.9 and at 223.5 nm were selected to determine dorzolamide and timolol maleate in the binary mixture. Calibration graphs were established for 8.0-30.0 microg ml(-1) for dorzolamide hydrochloride and 3.0-24.6 microg ml(-1) for timolol maleate in binary mixture. Good linearity, precision and selectivity were found, and the proposed methods were applied successfully to the pharmaceutical dosage from containing the above-mentioned drug combination without any interference by the excipients. Vierordt's method was also developed for a comparison method.

Description

Dorzolamide hydrochloride (L671152 Hcl; MK507 Hcl) is an anti-glaucoma agent, which is a carbonic anhydrase inhibitor.

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