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。
生物活性 | Acetazolamide is acarbonic anhydrase(CA)IXinhibitor with anIC50of 30 nM forhCA IX. Acetazolamide has diuretic, antihypertensive and anti-gonococcal activities[1][4][5][6]. |
IC50& Target | IC50: 30 nM (hCA IX), 130 nM (hCA II)[1] |
体外研究 (In Vitro) | Acetazolamide also inhibits hCA II with an IC50of 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].
|
体内研究 (In Vivo) | 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]. Acetazolamide (50 mg/kg; PO, for 3 days) significantly reduces the gonococcal load in the vagina of infected mice by 90%[6].
|
Clinical Trial | |
分子量 | |
性状 | |
Formula | |
CAS 号 | |
中文名称 | |
运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Powder | -20°C | 3 years | | 4°C | 2 years | In solvent | -80°C | 6 months | | -20°C | 1 month |
|
溶解性数据 | In Vitro: DMSO : 50 mg/mL(224.97 mM;Need ultrasonic) H2O : 1 mg/mL(4.50 mM;Need ultrasonic) 配制储备液 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 |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百 分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (11.25 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (11.25 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (11.25 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (11.25 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 3. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (11.25 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (11.25 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 4. 请依序添加每种溶剂: PBS Solubility: 1.96 mg/mL (8.82 mM); Clear solution; Need ultrasonic and warming and heat to 60℃ *以上所有助溶剂都可在本网站选购。
|