|N-(4-甲基-2-氨基磺酰基-Δ2-1,3,4-噻二唑-5-亚基)乙酰胺|CsnPharm

CAS No.: 554-57-4

Methazolamide/醋甲唑胺 Catalog No. CSN11393

Synonyms: L584601;CL 8490;Neptazane

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.

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技术信息

生物活性

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].
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 ... more >> Attikon University Hospital Recruiting Athens, Attiki, Greece, 12462 Contact: Paraskevi MATSOTA, MD, PhD 00302105832374 matsota@yahoo.gr Principal Investigator: PARASKEVI MATSOTA, MD, PHD Collapse <<
NCT02390284	Glaucoma	Phase 3	Recruiting	July 2019	United States, Florida ... more >> 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 Collapse <<

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参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 4.2324 mL
- 21.1621 mL
- 42.3241 mL
- 5 mM
- 0.8465 mL
- 4.2324 mL
- 8.4648 mL
- 10 mM
- 0.4232 mL
- 2.1162 mL
- 4.2324 mL

技术信息

CAS号

554-57-4

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C5H8N4O3S2

运输

蓝冰

分子量

236.27

别名

L584601;CL 8490;Neptazane;Methenamide;Neptazaneat;Naptazane;N-Methylacetazolamide;醋甲唑胺

溶解度

DMSO	425.0 mg/mL (1798.8 mM) warming
Water	insoluble

动物实验配方

IP	2% DMSO+water	8 mg/mL	clear
PO	0.5% CMC-Na	32 mg/mL	suspension

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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 ... more >> Attikon University Hospital Recruiting Athens, Attiki, Greece, 12462 Contact: Paraskevi MATSOTA, MD, PhD 00302105832374 matsota@yahoo.gr Principal Investigator: PARASKEVI MATSOTA, MD, PHD Collapse <<
NCT02390284	Glaucoma	Phase 3	Recruiting	July 2019	United States, Florida ... more >> 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 Collapse <<
NCT02463357	Mountain Sickness	Phase 4	Active, not recruiting	November 30, 2018	United States, Michigan ... more >> Alma College Alma, Michigan, United States, 48801 Collapse <<
NCT00257829	Cervical Cancer	Phase 2	Withdrawn(This study was close... more >>d due to lack of funding.) Collapse <<	-	-
NCT01702025	Physiological Function in Low ... more >>Oxygen Environment Collapse <<	Phase 1 Phase 2	Completed	-	United States, Colorado ... more >> Colorado State University, Dept. of Health and Exercise Science Fort Collins, Colorado, United States, 80523-1582 Collapse <<
NCT02758470	Hypoxia	Phase 4	Completed	-	Canada, British Columbia ... more >> University of British Columbia Kelowna, British Columbia, Canada, V1V 1V7 Collapse <<
NCT02760121	Altitude Sickness ... more >> Hypertension, Pulmonary Collapse <<	Phase 4	Completed	-	Canada, British Columbia ... more >> University of British Columbia Kelowna, British Columbia, Canada, V1V 1V7 Collapse <<
NCT01587027	Mountain Sickness	Phase 1	Completed	-	United States, Colorado ... more >> Medical Center of the Rockies Loveland, Colorado, United States, 80538 Collapse <<
NCT01702025	-	-	Completed	-	-
NCT01587027	-	-	Completed	-	-

Methazolamide/醋甲唑胺 Catalog No. CSN11393

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