Methazolamide | L584601 | Carbonic Anhydrase Inhibitor | AmBeed-信号通路专用抑制剂

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醋甲唑胺 /Methazolamide {[allProObj[0].p_purity_real_show]}

货号：A120295 同义名： L584601;CL 8490

Methazolamide is a carbonic anhydrase inhibitor with Ki of 50 nM, 14 nM and 36 nM for hCA I, hCA II and bCA IV isoforms, respectively.

Methazolamide 化学结构
CAS号：554-57-4

Methazolamide 3D分子结构
CAS号：554-57-4

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Methazolamide 纯度/质量文件产品仅供科研

货号：A120295 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

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碳酸酐酶亚型比较

产品名称	Carbonic Anhydrase ↓ ↑	Carbonic Anhydrase I ↓ ↑	Carbonic Anhydrase II ↓ ↑	Carbonic Anhydrase IV ↓ ↑	Carbonic Anhydrase IX ↓ ↑	Carbonic Anhydrase XII ↓ ↑	其他靶点	纯度
Topiramate	✔						Calcium Channel	98%
Dichlorphenamide	✔							98%
Mafenide Acetate	✔							98%
Benzenesulphonamide	✔							98%
Dorzolamide HCl		+ Carbonic anhydrase I, Ki: 6000 nM	++++ Carbonic anhydrase II, Ki: 1.9 nM	+++ Carbonic anhydrase IV, Ki: 31 nM				98%
Methazolamide		++ hCAI, Ki: 50 nM	+++ hCAII, Ki: 14 nM	++ bCAIV, Ki: 36 nM				98%
Tioxolone		+ CAI, Ki: 91 nM						98%
U-104					++ CAIX, Ki: 45.1 nM	++++ CAXII, Ki: 4.5 nM		98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Methazolamide 生物活性

靶点

Carbonic Anhydrase IV

bCAIV, Ki:36 nM
Carbonic Anhydrase I

hCAI, Ki:50 nM
Carbonic Anhydrase II

hCAII, Ki:14 nM

描述

Methazolamide (L584601) is a sulfonamide derivative used as a carbonic anhydrase inhibitor with a Ki of 14 nM for human carbonic anhydrase II^[3]. Methazolamide is an intraocular pressure-lowering drug that is used in the treatment of glaucoma and other ophthalmologic abnormalities^[4]. Methazolamide can increase systemic metabolic acidosis and sequentially improve ventilation and oxygenation level. In addition to the effect as a carbonic anhydrase inhibitor, methazolamide directly activates the transcription factor anti-oxidative nuclear factor-related factor 2 (Nrf2) and inhibits interleukin-1β (IL-1β) release. Methazolamide may thus represent an alternative for acetazolamide when taken for high-altitude illnesses prophylaxis and treatment^[5]. Methazolamide exhibits dose-dependent efficacy for the treatment of excessive erythrocytosis induced by long-term hypoxia^[6].

Methazolamide 临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT03165045	-		Active, not recruiting	January 31, 2019	-
NCT03362021	-		Recruiting	March 2019	Greece ... 展开 >> Attikon University Hospital Recruiting Athens, Attiki, Greece, 12462 Contact: Paraskevi MATSOTA, MD, PhD 00302105832374 matsota@yahoo.gr Principal Investigator: PARASKEVI MATSOTA, MD, PHD 收起 <<
NCT02390284	Glaucoma	Phase 3	Recruiting	July 2019	United States, Florida ... 展开 >> Bascom Palmer Eye Institute - University of Miami Recruiting Miami, Florida, United States, 33136 Contact: Marlene Perez, RC 305-482-4309 marlene.perez@med.miami.edu Contact: Shiva Roghaee, RA 305 482 4309 sxr935@med.miami.edu Principal Investigator: Vittorio Porciatti, DSc Sub-Investigator: John J McSoley, OD Sub-Investigator: Luis E Vazquez, MD,PhD Sub-Investigator: Steven J Gedde, MD Sub-Investigator: Pedro F Monsalve, RA Sub-Investigator: Maja Kostic, PhD 收起 <<

Methazolamide 参考文献

[1]Casini A, Antel J, et al. Carbonic anhydrase inhibitors: SAR and X-ray crystallographic study for the interaction of sugar sulfamates/sulfamides with isozymes I, II and IV. Bioorg Med Chem Lett. 2003 Mar 10;13(5):841-5.

[2]Kiwull-Schone HF, Li Y, et al. Methazolamide does not impair respiratory work performance in anesthetized rabbits. Am J Physiol Regul Integr Comp Physiol. 2009 Sep;297(3):R648-54.

[3]Abbate F, Casini A, Scozzafava A, Supuran CT. Carbonic anhydrase inhibitors: X-ray crystallographic structure of the adduct of human isozyme II with the perfluorobenzoyl analogue of methazolamide. Implications for the drug design of fluorinated inhibitors. J Enzyme Inhib Med Chem. 2003 Aug;18(4):303-8

[4]Yang F, Xuan J, Chen J, Zhong H, Luo H, Zhou P, Sun X, He L, Chen S, Cao Z, Luo X, Xing Q. HLA-B*59:01: a marker for Stevens-Johnson syndrome/toxic epidermal necrolysis caused by methazolamide in Han Chinese. Pharmacogenomics J. 2016 Feb;16(1):83-7

[5]Lu H, Zhang H, Jiang Y. Methazolamide in high-altitude illnesses. Eur J Pharm Sci. 2020 May 30;148:105326

[6]Zhang Z, Xiao Z, Deng B, Liu X, Liu W, Nie H, Li X, Chen Z, Yang D, Duan R. Therapeutic Efficacy of Methazolamide Against Intermittent Hypoxia-Induced Excessive Erythrocytosis in Rats. High Alt Med Biol. 2018 Mar;19(1):69-80

Methazolamide 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

4.23mL

0.85mL

0.42mL

21.16mL

4.23mL

2.12mL

42.32mL

8.46mL

4.23mL

Methazolamide 技术信息

CAS号	554-57-4
分子式	C₅H₈N₄O₃S₂
分子量	236.272

别名	L584601;CL 8490;N Methylacetazolamide;Naptazane;Neptazaneat;Methenamide;Neptazane
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,2-8°C

溶解度

DMSO: 50 mg/mL(211.62 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验配方

IP 2% DMSO+water 8 mg/mL clear

PO 0.5% CMC-Na 32 mg/mL suspension

临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT03165045	-		Active, not recruiting	January 31, 2019	-
NCT03362021	-		Recruiting	March 2019	Greece ... 展开 >> Attikon University Hospital Recruiting Athens, Attiki, Greece, 12462 Contact: Paraskevi MATSOTA, MD, PhD 00302105832374 matsota@yahoo.gr Principal Investigator: PARASKEVI MATSOTA, MD, PHD 收起 <<
NCT02390284	Glaucoma	Phase 3	Recruiting	July 2019	United States, Florida ... 展开 >> Bascom Palmer Eye Institute - University of Miami Recruiting Miami, Florida, United States, 33136 Contact: Marlene Perez, RC 305-482-4309 marlene.perez@med.miami.edu Contact: Shiva Roghaee, RA 305 482 4309 sxr935@med.miami.edu Principal Investigator: Vittorio Porciatti, DSc Sub-Investigator: John J McSoley, OD Sub-Investigator: Luis E Vazquez, MD,PhD Sub-Investigator: Steven J Gedde, MD Sub-Investigator: Pedro F Monsalve, RA Sub-Investigator: Maja Kostic, PhD 收起 <<
NCT02463357	Mountain Sickness	Phase 4	Active, not recruiting	November 30, 2018	United States, Michigan ... 展开 >> Alma College Alma, Michigan, United States, 48801 收起 <<
NCT00257829	Cervical Cancer	Phase 2	Withdrawn(This study was close... 展开 >>d due to lack of funding.) 收起 <<	-	-
NCT01702025	Physiological Function in Low ... 展开 >>Oxygen Environment 收起 <<	Phase 1 Phase 2	Completed	-	United States, Colorado ... 展开 >> Colorado State University, Dept. of Health and Exercise Science Fort Collins, Colorado, United States, 80523-1582 收起 <<
NCT02758470	Hypoxia	Phase 4	Completed	-	Canada, British Columbia ... 展开 >> University of British Columbia Kelowna, British Columbia, Canada, V1V 1V7 收起 <<
NCT02760121	Altitude Sickness ... 展开 >> Hypertension, Pulmonary 收起 <<	Phase 4	Completed	-	Canada, British Columbia ... 展开 >> University of British Columbia Kelowna, British Columbia, Canada, V1V 1V7 收起 <<
NCT01587027	Mountain Sickness	Phase 1	Completed	-	United States, Colorado ... 展开 >> Medical Center of the Rockies Loveland, Colorado, United States, 80538 收起 <<
NCT01702025	-		Completed	-	-
NCT01587027	-		Completed	-	-

醋甲唑胺 /Methazolamide {[allProObj[0].p_purity_real_show]}

Methazolamide 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

Methazolamide 质控信息

Methazolamide 生物活性

Methazolamide 临床研究

Methazolamide 参考文献

Methazolamide 实验方案

Methazolamide 技术信息

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Carbonic Anhydrase IV	bCAIV, Ki:36 nM
Carbonic Anhydrase I	hCAI, Ki:50 nM
Carbonic Anhydrase II	hCAII, Ki:14 nM

醋甲唑胺 /Methazolamide {[allProObj[0].p_purity_real_show]}

Methazolamide 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

Methazolamide 质控信息

Methazolamide 生物活性

Methazolamide 临床研究

Methazolamide 参考文献

Methazolamide 实验方案

Methazolamide 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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Methazolamide 纯度/质量文件产品仅供科研