Acetazolamide (Synonyms: 乙酰唑胺)
目录号: PL05411 纯度: ≥99%
CAS No. :59-66-5
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中文名称
Acetazolamide
中文别名
乙酰唑胺;N-[5-(氨磺酰基)-1,3,4-噻二唑-2-基]乙酰胺;17-氨基-3,6,9,12,15-五氧杂十七烷醇;醋唑磺胺;醋唑磺胺 EP标准品;醋唑磺胺系统适用性 EP标准品;三磷酸腺苷二钠(ATP);乙酰唑胺 USP标准品;乙酰唑胺 标准品;乙酰唑胺-13C2-D3;乙酰唑胺杂质;2-乙酰氨基-1,3,4-噻二唑-5-磺酰胺;ACET偶氮酰胺;阿昔洛韦杂质A;代马克司;代冒克斯;丹木斯
英文名称
Acetazolamide
英文别名
acetazolamide;2-acetamido-5-sulfamoyl-1,3,4-thiadiazole;2-acetylamino-1,3,4-thiadiazole-5-sulfonamide;5-acetamido-1,3,4-thiadiazole-2-sulfonamide;N-[5-(Aminosulfonyl)-1,3,4-thiadiazol-2-yl]acetamide;5-acetamido-1,3,4-thiadiazole-2-sulphonamide;Cidamex;DIACARB;Diakarb;Diamox;Didoc;Diluran;Donmox;Edemox;Glupax;N-(5-Sulfamoyl-1,3,4-thiadiazol-2-yl)acetamide;N-(5-[Aminosulfonyl]-1,3,4-thiadiazol-2-yl)acetamide;Acetazolamid;Glaupax;Defiltran;Nephramide;Acetamox;Phonurit;Nephramid;Dehydratin;Natrionex;Duiramid;Diuramid;Eumicton;Diutazol;Vetamox;Fonurit;SK-acetazolamide;Diuriwas;Acetozalamide;Acetazolamidum;Acetazolamida;Acetazoleamide;Diureticum-holzinger;Acetamidothiadiazolesulfonamide;Acetazolamine;Atenezol;Diamox Sequels;4-D;Glaumox;Acetazolamide (AAZ);5-acetylamino-1,3,4-thiadiazole-2-sulfonamide;MLS001148438;Q-200580;HMS3712A07;A832415;KBioGR_000558;ACETAZOLAMIDE [WHO-DD];Carbonic Anhydrase Inhibitor No. 6063;Acetazolamide Dioptic Brand;D88526;ACETAZOLAMIDE [EP MONOGRAPH];Acetazolamide [USP:INN:BAN:JAN];ACETAZOLAMIDE [VANDF];CARBONIC ANHYDRASE INHIBITOR NO 6063;NCGC00015074-08;1ydb;Acetazolamidum [INN-Latin];CS-3568;SPBio_000004;Acetazolamide, >=99%, powder;NSC-145177;Grin Brand of Acetazolamide;C4H6N4O3S2;NCGC00015074-10;HY-B0782;NC00491;ACETAZOLAMIDE [JAN];3hs4;Medphano Brand of Acetazolamide;Diuramide;NSC145177;LP00039;BCP29616;Acetazolamide for system suitability, European Pharmacopoeia (EP) Reference Standard;CAS-59-66-5;Pharmakon1600-01500102;Acetazolamide Medphano Brand;NCGC00015074-04;SPECTRUM1500102;Jumer Brand of Acetazolamide;Acetazolamide, AAZ;SMR000058394;ACETAZOLAMIDE [HSDB];SR-01000000065;Acetazolam;3czv;Lopac-A-6011;NCGC00015074-15;D0E1SW;EU-0100039;DivK1c_000017;C4-H6-N4-O3-S2;Acetazolamide (JP15/USP/INN);Tox21_110078;HMS500A19;N-[5-(aminosulfonyl)-1,3,5-thiadiazol-2-yl]acetamide;Acetazolamide Wassermann Brand;NCGC00015074-03;ACETAZOLAMIDE (MART.);Tox21_110078_1;Ak Zol;Diamox (TN);Acetazolamide [BAN:INN:JAN];ACETAZIDE;ICN Brand of Acetazolamide;Acetazolamide Llorens Brand;Acetazolamide [INN:BAN:JAN];SDCCGSBI-0050028.P005;3ucj;Chiesi Brand of Acetazolamide;CS-O-07116;Prestwick0_000003;HumaZolamide;Atenezo;O3FX965V0I;Acetazolamide, European Pharmacopoeia (EP) Reference Standard;2h4n;2xtk;BDBM10880;Acetazolamide Jumer Brand;3dc3;SPBio_001926;ACETAZOLAMIDE [INN];4g0c;ACETAZOLAMIDE [USP-RS];Spectrum4_000139;BRD-K43457670-001-22-9;N-(5-Sulfamoyl-[1,3,4]thiadiazol-2-yl)-acetamide;HMS1568A07;Llorens Brand of Acetazolamide;5-Acetamide-1,4-thiadiazole-2-sulfonamide;Storzolamide;Acetazolamide, analytical standard;s4506;ACETAZOLAMIDUM [WHO-IP LATIN];2uy4;NSC-755854;2-Acetylamino-1,3,4-thiadiazole-5-sulfonamide;BIDD:GT0643;IDI1_000017;ACETAZOLAMIDE [WHO-IP];BSPBio_001788;HMS3744A21;Dioptic Brand of Acetazolamide;Dazamide;ATENAZOL;Huma Zolamide;NCGC00015074-05;1azm;A 6011;HMS2232G23;1ydd;NCGC00023455-05;Monosodium Salt Acetazo...
Cas No.
59-66-5
分子式
C4H6N4O3S2
分子量
222.25
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
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 a carbonic anhydrase (CA) IX inhibitor with an IC 50 of 30 nM for hCA IX. Acetazolamide has diuretic, antihypertensive and anti-gonococcal activities.
性状
Solid
IC50 & Target[1][2]
IC50: 30 nM (hCA IX), 130 nM (hCA II)
体外研究(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
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.
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%. has not independently confirmed the accuracy of these methods. They are for reference only.
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
ClinicalTrial
参考文献
[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.
溶解度数据
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
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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