Methazolamide

Catalog No.S4039

Methazolamide is a carbonic anhydrase inhibitor with Ki of 50 nM, 14 nM and 36 nM for hCA I, hCA II and bCA IV isoforms, respectively.

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Methazolamide Chemical Structure

Methazolamide Chemical Structure
Molecular Weight: 236.27

Validation & Quality Control

Quality Control & MSDS

Product Information

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Product Description

Biological Activity

Description Methazolamide is a carbonic anhydrase inhibitor with Ki of 50 nM, 14 nM and 36 nM for hCA I, hCA II and bCA IV isoforms, respectively.
Targets hCAII [1] bCAIV [1] hCAI [1]
IC50 14 nM(Ki) 36 nM(Ki) 50 nM(Ki)
In vitro Methazolamide is a carbonic anhydrase inhibitor with Ki of 50 nM, 14 nM and 36 nM for hCA I, hCA II and bCA IV isoforms, respectively. [1] Methazolamide is of strength equal to acetazolamide, another carbonic anhydrase inhibitor used to treat irregular breathing disorders. However, methazolamide differs from acetazolamide in that it fails to activate Ca2+-dependent potassium channels in skeletal muscles. [2]
In vivo Methazolamide does not impair respiratory work performance in anesthetized rabbits. [2]
Features Methazolamide potently inhibits various isoforms of carbonic anhydrase.

Protocol(Only for Reference)

Kinase Assay: [3]

Spectrophotometric method A stopped flow variant of the Pocker and Stone spectrophotometric method has been employed, using an SX.18MV-R Applied Photophysics stopped flow instrument.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Casini A, et al. Bioorg Med Chem Lett, 2003, 13(5), 841-845.

[2] Kiwull-Sch?ne HF, et al. Am J Physiol Regul Integr Comp Physiol, 2009, 297(3), R648-654.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-05-07)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02758470 Not yet recruiting Hypoxia University of British Columbia September 2016 Phase 4
NCT02760121 Not yet recruiting Altitude Sickness|Hypertension, Pulmonary University of British Columbia June 2016 Phase 4
NCT02463357 Recruiting Mountain Sickness University of Colorado, Denver|Alma College August 2015 Phase 4
NCT02390284 Recruiting Glaucoma University of Miami|National Eye Institute (NEI) September 2014 Phase 3
NCT01702025 Completed Physiological Function in Low Oxygen Environment Colorado State University|Defense Advanced Research Proje  ...more Colorado State University|Defense Advanced Research Projects Agency|University of Colorado, Denver June 2012 Phase 1|Phase 2

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Chemical Information

Download Methazolamide SDF
Molecular Weight (MW) 236.27
Formula

C5H8N4O3S2

CAS No. 554-57-4
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms CL 8490
Solubility (25°C) * In vitro DMSO 47 mg/mL (198.92 mM)
Ethanol 3 mg/mL (12.69 mM)
Water <1 mg/mL (<1 mM)
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name Acetamide, N-[5-(aminosulfonyl)-3-methyl-1,3,4-thiadiazol-2(3H)-ylidene]-

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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