215902-M
Carbonic Anhydrase IX Inhibitor III, Methazolamide
The Carbonic Anhydrase IX Inhibitor III, Methazolamide, also referenced under CAS 554-57-4, controls the biological activity of Carbonic Anhydrase IX.
别名:
Carbonic Anhydrase IX Inhibitor III, Methazolamide, N-[5-(aminosulfonyl)-3-methyl-1,3,4-thiadiazol-2(3H)-ylidene]acetamide, Carbonic Anhydrase Inhibitor, Methazolamide, CAIX Inhibitor III
InChI
1S/C5H8N4O3S2/c1-3(10)7-4-9(2)8-5(13-4)14(6,11)12/h1-2H3,(H2,6,11,12)
InChI key
FLOSMHQXBMRNHR-UHFFFAOYSA-N
assay
≥99% (HPLC)
form
powder
potency
20 nM Ki
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
white
solubility
DMSO: 50 mg/mL
General description
A cell-permeable thiadiazolylsulfonamide derivative that acts as a carbonic anhydrase (CA) inhibitor (Ki = 20 nM) with anti-glaucoma, anti-diabetic, and potential anti-neoplastic activity. May induce death in hypoxic tumor cells by inhibiting tumor-associated CAIX in maintaining an acidic tumor microenvironment, and blocking CAIX-dependent resistance to chemotherapy in these tumors. Shown to enhance insulin sensitivity and reduce HbA1c levels in diabetic rodent models in a dose-dependent manner. Shown to reduce oxygen and glucose-deprived cell death in primary cerebrocortical neurons by diminishing the release of cytochrome c and dissipating the mitochondrial membrane potential gradient.
Biochem/physiol Actions
Primary Target
carbonic anhydrase
carbonic anhydrase
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Maren, T., et al. 1977. Invest Ophthalmol Vis Sci.16, 730.
Chegwidden, W. R. and Spencer, I. M. 1995. Inflammopharmacology.3, 231.
Wang, X., et al. 2009. Stroke.40, 1877.
Konstantopoulos, N., et al. 2012. Diabetes.
Chegwidden, W. R. and Spencer, I. M. 1995. Inflammopharmacology.3, 231.
Wang, X., et al. 2009. Stroke.40, 1877.
Konstantopoulos, N., et al. 2012. Diabetes.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
signalword
Warning
hcodes
Hazard Classifications
Acute Tox. 4 Dermal - Acute Tox. 4 Inhalation - Acute Tox. 4 Oral - Carc. 2
存储类别
11 - Combustible Solids
wgk
WGK 3
法规信息
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