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CAS No. : 59-66-5
MCE 国际站:Acetazolamide
产品活性:Acetazolamide 是一种碳酸酐酶 (CA) IX 抑制剂,对 hCA IX 的 IC50 为 30 nM。Acetazolamide 具有利尿、抗高血压和抗淋球菌活性。
研究领域:Metabolic Enzyme/Protease | Autophagy | Anti-infection
作用靶点:Carbonic Anhydrase | Autophagy | Bacterial
In Vitro: Acetazolamide also inhibits hCA II with an IC50 of 130 nM.
Acetazolamide (Ace) is a small heteroaromatic sulfonamide that binds to various carbonic anhydrases with high affinity, acting as a carbonic anhydrase (CA) inhibitor.
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.
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.
Combined Ace and Cis treatment effectively promotes apoptosis in Hep-2 cells.
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.
In Vivo: Acetazolamide (40 mg/kg) significantly potentiates the inhibitory effect of MS-275 on tumorigenesis in neuroblastoma (NB) SH-SY5Y xenografts.
Acetazolamide (40 mg/kg) and/or MS-275 treatment reduce expression of HIF1-α and CAIX in NB SH-SY5Y xenograft.
Acetazolamide (40 mg/kg), MS-275 and Acetazolamide+MS-275 reduce expression of mitotic and proliferative markers in NB SH-SY5Y xenografts.
Acetazolamide (50 mg/kg; PO, for 3 days) significantly reduces the gonococcal load in the vagina of infected mice by 90%.
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