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| 100mg |
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| 500mg |
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| 5g |
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Methazolamide (Neptazaneat; Naptazane; CL-8490; CL8490) is a highly potent and selective inhibitor of carbonic anhydrase (CAI) with important biological activity. It inhibits the isoforms of CA such as hCA I, hCA II and bCA IV with Ki of 50 nM, 14 nM and 36 nM, respectively. Methazolamide is used to glaucoma (to lower the intraocular pressure inside the eyes).
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| References |
Bioorg Med Chem Lett.2003;13(5):841-5;Am J Physiol Regul Integr Comp Physiol.2009;297(3):R648-54.
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| Additional Infomation |
Methazolamide is a member of thiadiazoles and a sulfonamide.
A carbonic anhydrase inhibitor that is used as a diuretic and in the treatment of glaucoma. See also: Methazolamide (annotation moved to). |
| Molecular Formula |
C5H8N4O3S2
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| Molecular Weight |
236.27
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| Exact Mass |
236.003
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| CAS # |
554-57-4
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| Related CAS # |
Methazolamide-d6;1795142-30-1
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| PubChem CID |
4100
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| Appearance |
White to off-white solid powder
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| Density |
1.8±0.1 g/cm3
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| Boiling Point |
402.0±28.0 °C at 760 mmHg
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| Melting Point |
208ºC (dec.)
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| Flash Point |
196.9±24.0 °C
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| Vapour Pressure |
0.0±0.9 mmHg at 25°C
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| Index of Refraction |
1.737
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| LogP |
0.13
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
14
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| Complexity |
419
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
FLOSMHQXBMRNHR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C5H8N4O3S2/c1-3(10)7-4-9(2)8-5(13-4)14(6,11)12/h1-2H3,(H2,6,11,12)
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| Chemical Name |
N-(3-methyl-5-sulfamoyl-1,3,4-thiadiazol-2-ylidene)acetamide
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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: This product requires protection from light (avoid light exposure) during transportation and storage. |
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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 (10.58 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 (10.58 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 (10.58 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.2324 mL | 21.1622 mL | 42.3245 mL | |
| 5 mM | 0.8465 mL | 4.2324 mL | 8.4649 mL | |
| 10 mM | 0.4232 mL | 2.1162 mL | 4.2324 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 |
| NCT05498103 | Recruiting | Drug: Methazolamide 25 MG Drug: Methazolamide 50 MG |
Glaucoma, Open-Angle | University of Colorado, Denver | February 17, 2023 | Phase 4 |
| NCT06312800 | Withdrawn | Drug: Placebo Drug: Methazolamide |
Essential Tremor | Henry Ford Health System | March 2016 | Phase 2 |
| NCT01587027 | Completed Has Results | Drug: Aminophylline Drug: Methazolamide |
Mountain Sickness | Poudre Valley Health System | December 2011 | Phase 1 |
| NCT05575180 | Completed | Drug: Acetazolamide 250Mg Tab Drug: Methazolamide Pill |
High Altitude Effects | University of Waterloo | August 11, 2023 | Phase 4 |
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