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Purity: ≥98%
Dorzolamide HCl (also known as MK-507; L-671152 HCl; L671152; MK507; trade name Trusopt), an anti-glaucoma agent and CAI (carbonic anhydrase inhibitors), is a water-soluble and potent inhibitor of human carbonic anhydrase II and IV with Ki of 1.9 nM and 31 nM, respectively. Dorzolamide wa approved for use as an 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.
| ln Vitro |
Dorzolamide hydrochloride inhibits Component A, which is brought on by the CO2 inflow and the hydration of CA-II that follows, in a dose-dependent manner with an IC50 of 2.4 μM [2].
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| ln Vivo |
In an EAC solid tumor model, dorzolamide hydrochloride (3, 10, or 30 mg/kg/day, i.p.) has anticancer efficacy in conjunction with mitomycin C. The calculated ratios (relative values 57.3±1, 25.5±1.8, and 24.3±0.7%, respectively) were dose-dependently lowered by dorzolamide hydrochloride [3].
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| Animal Protocol |
Animal/Disease Models: Female Swiss albino mice (EAC solid tumor)[3].
Doses: 3, 10, or 30 mg/kg/day (synergized mitomycin C). Route of Administration: IP, daily for 3 weeks. Experimental Results: Upregulated TXNIP and p53 while downregulated bcl-2. Effective in retarding the growth of EAC in mice. |
| References |
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| Additional Infomation |
Dorzolamide Hydrochloride is the hydrochloride salt form of dorzolamide, an inhibitor of carbonic anhydrase, a zinc-containing enzyme that catalyzes the rapid conversion of carbon dioxide and water into carbonic acid, protons and bicarbonate ions. Distributed throughout many cells and tissues, various carbonic anhydrases play important roles in mineral and metabolic homeostasis. (NCI04)
See also: Dorzolamide (has active moiety); Dorzolamide Hydrochloride; Timolol Maleate (component of). |
| Molecular Formula |
C10H16N2O4S3.HCL
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| Molecular Weight |
360.9
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| Exact Mass |
360.004
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| CAS # |
130693-82-2
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| Related CAS # |
Dorzolamide;120279-96-1
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| PubChem CID |
6918132
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| Appearance |
White to off-white solid powder
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| Density |
1.53 g/cm3
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| Boiling Point |
575.8ºC at 760 mmHg
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| Melting Point |
283-285ºC
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| Flash Point |
302ºC
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| Vapour Pressure |
2.93E-13mmHg at 25°C
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| LogP |
4.666
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
20
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| Complexity |
534
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| Defined Atom Stereocenter Count |
2
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| SMILES |
CCN[C@H]1C[C@@H](S(=O)(=O)C2=C1C=C(S2)S(=O)(=O)N)C.Cl
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| InChi Key |
OSRUSFPMRGDLAG-QMGYSKNISA-N
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| InChi Code |
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
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| Chemical Name |
(4S,6S)-4-(ethylamino)-6-methyl-7,7-dioxo-5,6-dihydro-4H-thieno[2,3-b]thiopyran-2-sulfonamide;hydrochloride
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.93 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.93 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.93 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 11 mg/mL (30.48 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05973305 | Completed | Drug: Dorzol 20 mg/ml Drug: Trusopt 20 mg/ml |
Primary Open Angle Glaucoma of Both Eyes |
Jadran Galenski laboratorij d.d. | April 5, 2017 | Phase 3 |
| NCT05857267 | Recruiting | Drug: Dorzolamide / Timolol Ophthalmic Solution |
Glaucoma, Open-Angle Ocular Hypertension |
Laboratorios Poen | March 7, 2023 | Phase 4 |
| NCT00832377 | Completed Has Results | Drug: timolol/dorzolamide combination | Glaucoma | Merck Sharp & Dohme LLC | April 24, 2009 | Phase 2 |
| NCT06369077 | Recruiting NEW | Drug: dorzolamide/timolol | Glaucoma, Open-Angle Glaucoma; Drugs |
CT Glaucoma Associates | April 2024 | Phase 4 |
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