Acetazolamide

Catalog No.S4506 Batch:S450601

Technical Data

Formula	C₄H₆N₄O₃S₂
Molecular Weight	222.25	CAS No.	59-66-5
Solubility (25°C)*	In vitro	DMSO	44 mg/mL (197.97 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description

Acetazolamide (Diamox), a potent carbonic anhydrase (CA) inhibitor, is commonly used in clinical practice as an immediate and readily available option for acute reduction of intraocular pressure(IOP).

Targets

Carbonic anhydrase ^[4]

10 nM

In vitro

acetazolamide reduces invasiveness of cancer cells in vitro^[3].

In vivo

Acetazolamide reduces inflammation-induced heat hyperalgesia, probably acting both peripherally and centrally^[1]. Acetazolamide shows significant inhibitory effect on angiogenesis in CAM and endothelial cell proliferation^[2]. Acetazolamide is clinically used to reduce intraocular pressure in glaucoma, to correct metabolic alkalosis, and to manage cerebral edema. Its treatment may also be beneficial as an adjunct to cancer chemotherapy, because it can produce additive tumor growth delays with anticancer drugs in vivo^[3].

Protocol (from reference)

Cell Assay:^{^[3]}	Cell lines renal carcinoma cell lines(Caki-1, Caki-2, ACHN, and A-498) Concentrations 10 μM Incubation Time 48 h Method The invasion assay is performed in a Biocoat Matrigel invasion chamber. Cells (n = 1.8 × 10⁵) are added to the chamber and cultured for 48 h in the presence or absence of acetazolamide, which was administered twice during the 48-h period: the first dose at the beginning of the assay and the second after 24 h. After growing for 48 h, noninvasive cells are removed from the upper surface of the membrane with a cotton swab. The invasive cells on the lower surface of the membrane are fixed with 4% (vol/vol) neutral-buffered formaldehyde, stained with toluidine blue, and counted in 20 separate areas with a Leitz Diaplan microscope.
Animal Study:^{^[1]}	Animal Models Male Sprague-Dawley rats Dosages 10, 100, 200 mg/kg Administration i.p.

Cell Assay:^{^[3]}

Cell lines
renal carcinoma cell lines(Caki-1, Caki-2, ACHN, and A-498)
Concentrations
10 μM
Incubation Time
48 h
Method
The invasion assay is performed in a Biocoat Matrigel invasion chamber. Cells (n = 1.8 × 10⁵) are added to the chamber and cultured for 48 h in the presence or absence of acetazolamide, which was administered twice during the 48-h period: the first dose at the beginning of the assay and the second after 24 h. After growing for 48 h, noninvasive cells are removed from the upper surface of the membrane with a cotton swab. The invasive cells on the lower surface of the membrane are fixed with 4% (vol/vol) neutral-buffered formaldehyde, stained with toluidine blue, and counted in 20 separate areas with a Leitz Diaplan microscope.

Animal Study:^{^[1]}

Animal Models
Male Sprague-Dawley rats
Dosages
10, 100, 200 mg/kg
Administration
i.p.

References

[4] Hardman, J.G., et al. Goodman and Gilman's The Pharmacological Basis of Therapeutics. 9th ed. New York, NY: McGraw-Hill, 1996, p. 693.

+ Expand

Selleck's Acetazolamide has been cited by 6 publications

Novel energy optimizer, meldonium, rapidly restores acute hypobaric hypoxia-induced brain injury by targeting phosphoglycerate kinase 1 [ Cell Commun Signal, 2024, 22(1):383]	PubMed: 39075489
Carbonic anhydrase inhibitor alleviates retinal barrier toxicity in paclitaxel-induced retinopathy and macular edema by inhibiting CAXIV [ Int Ophthalmol, 2024, 44(1):437]	PubMed: 39578251
Eleutheroside B ameliorated high altitude pulmonary edema by attenuating ferroptosis and necroptosis through Nrf2-antioxidant response signaling [ Biomed Pharmacother, 2022, 156:113982]	PubMed: 36411652
The carbonic anhydrase inhibitor acetazolamide inhibits urinary bladder cancers via suppression of β-catenin signaling [ Cancer Sci, 2022, 113(8):2642-2653]	PubMed: 35723039
Meldonium Ameliorates Hypoxia-Induced Lung Injury and Oxidative Stress by Regulating Platelet-Type Phosphofructokinase-Mediated Glycolysis [ Front Pharmacol, 2022, 13:863451]	PubMed: 35450040
Effect of cGMP-activated aquaporin 1 on TRPV4 in rats with allodynia induced by chronic compression of the dorsal root ganglion. [ Neurosci Lett, 2019, 10.1016/j.neulet.2019.134630]	PubMed: 31790718

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SHIPPING AND STORAGE
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