Acetazolamide (Synonyms: L-579,486, NSC 145177) |
| Katalog-Nr.GC11567 |
Acetazolamid ist ein Carboanhydrase (CA) IX-Hemmer mit einem IC50-Wert von 30 nM fÜr hCA IX.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 59-66-5
Sample solution is provided at 25 µL, 10mM.
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Acetazolamide is a carbonic anhydrase (CA) IX inhibitor with an IC50 of 30 nM for hCA IX[1]. Diuretic effects[4].
Acetazolamide also inhibits hCA II with an IC50 of 130 nM[1].
Acetazolamide (Ace) is a small heteroaromatic sulfonamide that binds to various carbonic anhydrases with high affinity, acting as a carbonic anhydrase (CA) inhibitor[2].
Compared with the control group, the high Acetazolamide concentration (AceH, 50 nM), Cisplatin (Cis; 1 µg/mL) and Cis combined with the low Acetazolamide concentration (AceL, 10 nM) treatments significantly reduces viability of Hep-2 cells[2].
Treatment with the Acetazolamide/Cis combination significantly increases the expression levels of P53, as both AceL+Cis and AceH+Cis treatments result in significantly increased P53 protein expression levels compared with the control group. The Ace/Cis combination treatment significantly reduces the bcl-2/bax expression ratio, and increases the expression of caspase-3 protein, compared with the control group. AceL, AceH, Cis and AceL+Cis treatments significantly reduce the bcl-2/bax ratio compared with the control group[2].
Combined Ace and Cis treatment effectively promotes apoptosis in Hep-2 cells[2].
Combined treatment with Ace/Cis markedly decreases the expression of AQP1 mRNA in Hep-2 cells. Both AceH and AceL+Cis treatments decrease the expression of aquaporin-1 (AQP1) mRNA in Hep-2 cells compared with the control group[2].
Acetazolamide (40 mg/kg) significantly potentiates the inhibitory effect of MS-275 on tumorigenesis in neuroblastoma (NB) SH-SY5Y xenografts[3].
Acetazolamide (40 mg/kg) and/or MS-275 treatment reduce expression of HIF1-α and CAIX in NB SH-SY5Y xenograft[3].
Acetazolamide (40 mg/kg), MS-275 and Acetazolamide+MS-275 reduce expression of mitotic and proliferative markers in NB SH-SY5Y xenografts[3].
Reference:
[1]. Hou Z, et al. Dual-tail approach to discovery of novel carbonic anhydrase IX inhibitors by simultaneously matching the hydrophobic and hydrophilic halves of the active site. Eur J Med Chem. 2017 May 26;132:1-10.
[2]. Bayat Mokhtari R, et al. Acetazolamide potentiates the anti-tumor potential of HDACi, MS-275, in neuroblastoma. BMC Cancer. 2017 Feb 24;17(1):156.
[3]. Gao H, et al. Combined treatment with acetazolamide and cisplatin enhances chemosensitivity in laryngeal carcinoma Hep-2 cells. Oncol Lett. 2018 Jun;15(6):9299-9306.
[4]. Kassamali R, et al. Acetazolamide: a forgotten diuretic agent. Cardiol Rev. 2011 Nov-Dec;19(6):276-8.
Cell experiment: | Cell Viability Assay[2]Cell line: Hep-2 cells and HUVECsConcentration: 10 nM and 50 nMIncubation time: 48 hAssay: The cell viability of Hep-2 cells and HUVECs is measured by MTT assay. Hep-2 cells and HUVECs in logarithmic growth phase are plated in 96-well plates. Following 48 h of drug treatment as indicated, 200 µL MTT (5 mg/mL) is added to each well. Cells are incubated with the MTT solution at 37°C for 4 h. Then, 150 µL DMSO is added for 5 min. The optical density (OD) values are measured at 490 nm with a Versamax Microplate reader.Note: Combined treatment effectively reduced viability in Hep-2 cells. |
Animal experiment: | In vivo studies[3]Animal model: 4-6 weeks-old female NOD/SCID miceDosage: 40 mg/kg, intraperitoneal injection, every day for 2 weeksAdministration: Mice are randomized into four groups (5 mice per group). The control and treatment groups receive intraperitoneal injections of vehicle (PBS) or Acetazolamide (40 mg/kg), MS-275 (20 mg/kg) or the combination, respectively, every day for 2 weeks. Experiments are terminated when tumor sizes exceed 2 cm3 in volume or animals show signs of morbidity. Tumor diameters are measured on a daily basis until termination. Note: Inhibited tumor growth of NB xenografts with significant anti-tumor growth potentiation effect. |
References: [1]. Hou Z, et al. Dual-tail approach to discovery of novel carbonic anhydrase IX inhibitors by simultaneously matching the hydrophobic and hydrophilic halves of the active site. Eur J Med Chem. 2017 May 26;132:1-10. | |
| Cas No. | 59-66-5 | SDF | |
| Überlieferungen | L-579,486, NSC 145177 | ||
| Chemical Name | (Z)-N-(5-sulfamoyl-1,3,4-thiadiazol-2-yl)acetimidic acid | ||
| Canonical SMILES | C/C(O)=N/C1=NN=C(S(N)(=O)=O)S1 | ||
| Formula | C4H6N4O3S2 | M.Wt | 222.25 |
| Löslichkeit | ≥ 22.2mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.4994 mL | 22.4972 mL | 44.9944 mL |
| 5 mM | 0.8999 mL | 4.4994 mL | 8.9989 mL |
| 10 mM | 0.4499 mL | 2.2497 mL | 4.4994 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
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- Purity: >99.50%
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Average Rating: 5 (Based on Reviews and 24 reference(s) in Google Scholar.)
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