Rasagiline Mesylate | TVP1012 mesylate | MAO Inhibitor | AmBeed-信号通路专用抑制剂

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甲磺酸雷沙吉兰 /Rasagiline Mesylate {[allProObj[0].p_purity_real_show]}

货号：A262921 同义名： TVP1012 mesylate;(R)-AGN1135 mesylate

Rasagiline Mesylate is an irreversible and selective MAO-B inhibitor used in early Parkinson's disease.

Rasagiline Mesylate 化学结构
CAS号：161735-79-1

Rasagiline Mesylate 3D分子结构
CAS号：161735-79-1

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Rasagiline Mesylate 纯度/质量文件产品仅供科研

货号：A262921 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

全球学术期刊中引用的产品: • Cell, 2024, 101755. Ambeed. [ A399663 ]; • EMBO J., 2024. Ambeed. [ A295334 ]; • JMC, 2024, 67(20): 18265-18289. Ambeed. [ A538667 , A341145 , A117430 , A172297 ]; • JMC, 2024. Ambeed. [ A210558 , A1518164 ]; • Cell Death Discov., 2024, 10, 436. Ambeed. [ A384235 ]; 更多 >

MAO 亚型比较

产品名称	MAO ↓ ↑	MAO-A ↓ ↑	MAO-B ↓ ↑	纯度
Sennoside A	++ MAO, IC50: 17 μM			98%+
Glycyrrhizic acid	++++ MAO, IC50: 0.16 μM			80% HPLC
Rasagiline		++++ MAO-A, IC50: 412 nM	++++ MAO-B, IC50: 4.43 nM	99+%
Isatin	++ MAO, IC50: 15 μM	+ MAO-A, IC50: 58 μM	++ MAO-B, IC50: 14 μM	98%
Paeonol		+ MAO-A, IC50: 54.6 μM	+ MAO-B, IC50: 42.5 μM	98%
Tranylcypromine hydrochloride		+++ MAO-A, IC50: 11.5 μM	+++ MAO-B, IC50: 7 μM	97%
Moclobemide		+++ MAO-A (5-HT), IC50: 6.1 μM		99%+
Pargyline HCl		++ MAO-A, Ki: 13 μM	+++ MAO-B, Ki: 0.5 μM	99%+
Safinamide			++++ MAO-B, IC50: 98 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。

Rasagiline Mesylate 生物活性

描述

Rasagiline mesylate is a highly potent selective irreversible mitochondrial monoamine oxidase (MAO) inhibitor with IC50s of 4.43 nM and 412 nM for rat brain MAO B and A activity, respectively. The ED(50) values for ex vivo inhibition of MAO in the brain and liver by a single dose of rasagiline are 0.1+/-0.01, 0.042+/-0.0045 mg/kg respectively for MAO-B, and 6.48+/-0.81, 2.38+/-0.35 mg/kg respectively for MAO-A. Rasagiline was three to 15 times more potent than selegiline for inhibition of MAO-B in rat brain and liver in vivo on acute and chronic administration, but had similar potency in vitro^[3]. Rasagiline improves motor fluctuations and Parkinson disease (PD) symptoms in levodopa-treated PD patients^[4]. Rasagiline (up to 2 mg/day) has a good safety profile and a beneficial clinical effect in fluctuating patients with PD when given as an add-on to chronic levodopa therapy^[5]. Moreover, Rasagiline Mesylate has a positive effect in the post-MI (myocardial infarction) period with a significant attenuation in cardiac remodelling^[6].

Rasagiline Mesylate 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
NCT01280123	Parkinson's Disease	Phase 2	Completed	-	-
NCT01280123	-		Completed	-	-
NCT01155466	Parkinson Disease	Phase 3	Completed	-	-

Rasagiline Mesylate 参考文献

[1]Maruyama W, Akao Y, et al. Transfection-enforced Bcl-2 overexpression and an anti-Parkinson drug, rasagiline, prevent nuclear accumulation of glyceraldehyde-3-phosphate dehydrogenase induced by an endogenous dopaminergic neurotoxin, N-methyl(R)salsolinol. J Neurochem. 2001 Aug;78(4):727-35.

[2]Youdim MB, Gross A, Finberg JP. Rasagiline [N-propargyl-1R(+)-aminoindan] , a selective and potent inhibitor of mitochondrial monoamine oxidase B. Br J Pharmacol. 2001 Jan;132(2):500-6.

[3]Youdim MB, Gross A, Finberg JP. Rasagiline [N-propargyl-1R(+)-aminoindan], a selective and potent inhibitor of mitochondrial monoamine oxidase B. Br J Pharmacol. 2001 Jan;132(2):500-6

[4]Parkinson Study Group. A randomized placebo-controlled trial of rasagiline in levodopa-treated patients with Parkinson disease and motor fluctuations: the PRESTO study. Arch Neurol. 2005 Feb;62(2):241-8

[5]Rabey JM, Sagi I, Huberman M, Melamed E, Korczyn A, Giladi N, Inzelberg R, Djaldetti R, Klein C, Berecz G; Rasagiline Study Group. Rasagiline mesylate, a new MAO-B inhibitor for the treatment of Parkinson's disease: a double-blind study as adjunctive therapy to levodopa. Clin Neuropharmacol. 2000 Nov-Dec;23(6):324-30

[6]Varela A, Mavroidis M, Katsimpoulas M, Sfiroera I, Kappa N, Mesa A, Kostomitsopoulos NG, Cokkinos DV. The neuroprotective agent Rasagiline mesylate attenuates cardiac remodeling after experimental myocardial infarction. ESC Heart Fail. 2017 Aug;4(3):331-340

Rasagiline Mesylate 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

3.74mL

0.75mL

0.37mL

18.70mL

3.74mL

1.87mL

37.40mL

7.48mL

3.74mL

Rasagiline Mesylate 技术信息

CAS号	161735-79-1
分子式	C₁₃H₁₇NO₃S
分子量	267.344

别名	TVP1012 mesylate;(R)-AGN1135 mesylate
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,Room Temperature

溶解度

H₂O: 25 mg/mL(93.51 mM)，配合低频超声助溶

动物实验配方

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

NCT01280123	Parkinson's Disease	Phase 2	Completed	-	-
NCT01280123	-		Completed	-	-
NCT01155466	Parkinson Disease	Phase 3	Completed	-	-
NCT01155479	Parkinson Disease	Phase 3	Terminated(Termininated for bu... 展开 >>siness reasons) 收起 <<	-	-
NCT02696512	Brain Injury	Phase 1 Phase 2	Unknown	April 2017	United States, New Jersey ... 展开 >> International Brain Research Foundation Recruiting Edison, New Jersey, United States, 08837 Contact: Philip Defina, PhD 732-494-7600 pdefina@ibrfinc.org Principal Investigator: Philip Defina, PhD 收起 <<
NCT01155466	-		Completed	-	-
NCT03329508	Parkinson Disease	Phase 3	Recruiting	December 30, 2019	-
NCT01155479	-		Terminated(Termininated for bu... 展开 >>siness reasons) 收起 <<	-	-
NCT01215227	Parkinson Disease ... 展开 >> Idiopathic Parkinson Disease 收起 <<	Phase 3	Terminated	-	-
NCT01098396	-		Unknown	-	-
NCT00203125	Parkinson's Disease	Phase 3	Completed	-	-
NCT01968460	Parkinson's Disease	Phase 2 Phase 3	Completed	-	-
NCT02789020	Parkinson's Disease	Phase 2	Recruiting	December 2020	United States, Florida ... 展开 >> Laboratory for Rehabilitation Neuroscience Recruiting Gainesville, Florida, United States, 32611 Contact: Nieci Black 352-294-1771 nblack@ufl.edu 收起 <<
NCT00902941	Parkinson´s Disease	Phase 4	Completed	-	Germany ... 展开 >> University of Dresden Medical School, Smell & Taste Centre, Dept. of Neurology Dresden, Germany, 01307 收起 <<
NCT01215227	-		Terminated	-	-
NCT01532128	Parkinson Disease	Phase 1	Completed	-	France ... 展开 >> BIOTRIAL Rennes, France, F-35000 收起 <<
NCT02207387	Parkinson's Disease	Not Applicable	Unknown	March 2017	Canada, British Columbia ... 展开 >> Pacific Parkinson's Research Centre Recruiting Vancouver, British Columbia, Canada, V6P 2Z9 Principal Investigator: Martin J McKeown, MD 收起 <<
NCT00203060	Parkinson's Disease	Phase 3	Completed	-	-
NCT01048229	Early-stage Parkinson's Diseas... 展开 >>e 收起 <<	Phase 4	Terminated(recruitment)	-	-
NCT00492336	Schizophrenia	Phase 4	Completed	-	United States, Maryland ... 展开 >> Baltimore VA Medical Center Baltimore, Maryland, United States, 21201 Keypoint Mental health Center Catonsville, Maryland, United States, 21228 Maryland Psychiatric REsearch Center Catonsville, Maryland, United States, 21228 Mosaic Community Mental health Center Catonsville, Maryland, United States, 21228 Keypoint Mental health Center Dundalk, Maryland, United States, 21222 收起 <<
NCT00104273	Dementia Alzh... 展开 >>eimer's Disease 收起 <<	Phase 2	Completed	-	-
NCT00492336	-		Completed	-	-
NCT00256204	Parkinson's Disease	Phase 3	Completed	-	-
NCT00256204	-		Completed	-	-
NCT00203034	Parkinson's Disease	Phase 3	Completed	-	United States, Illinois ... 展开 >> Rush - Presbyterian St. Luke's Medical Center Chicago, Illinois, United States, 60612 United States, New York Columbia - Presbyterian Medical Center New York, New York, United States, 10032 University of Rochester Rochester, New York, United States, 14642 United States, Texas Baylor College of Medicine Houston, Texas, United States, 77030 收起 <<
NCT02359552	Alzheimer's Disease	Phase 2	Active, not recruiting	February 15, 2019	United States, Nevada ... 展开 >> Cleveland Clinic Lou Ruvo Center for Brain Health Las Vegas, Nevada, United States, 89106 United States, Ohio Cleveland Clinic Main Campus Cleveland, Ohio, United States, 44195 Cleveland Clinic Lakewood Hospital Lakewood, Ohio, United States, 44107 收起 <<
NCT02068625	Retinal Detachment	Phase 4	Active, not recruiting	December 31, 2018	Switzerland ... 展开 >> Department of Ophthalmology, Bern University Hospital Bern, Switzerland, 3010 收起 <<
NCT01382342	Parkinson's Disease	Phase 4	Completed	-	United States, Rhode Island ... 展开 >> Butler Hospital Providence, Rhode Island, United States, 02906 收起 <<
NCT01765257	Drug-naïve Patients With Parki... 展开 >>nson's Disease Apathy 收起 <<	Phase 4	Unknown	March 2015	France ... 展开 >> CHU Clermont-Ferrand Not yet recruiting Clermont-Ferrand, France, 63003 Contact: Patrick LACARIN 04 73 75 11 95 placarin@chu-clermontferrand.fr 收起 <<
NCT01049984	Parkinson's Disease	Phase 4	Completed	-	-
NCT00203138	Parkinson's Disease	Phase 3	Completed	-	-
NCT01532128	-		Completed	-	-
NCT01055379	Depressive Symptoms ... 展开 >> Parkinson's Disease 收起 <<	Phase 4	Completed	-	Italy ... 展开 >> IT010 Cagliari, Italy, 9134 IT007 Chieti, Italy, 66013 IT004 Genova, Italy, 16132 IT005 Lido di Camaiore, Italy, 55043 IT003 Messina, Italy, 98122 IT012 Milano, Italy, 20135 IT001 Naples, Italy, 80131 IT011 Roma, Italy, 161 IT008 Rome, Italy, 133 IT015 Torino, Italy, 10126 IT013 Venezia, Italy, 30126 IT009 Verona, Italy, 37134 收起 <<
NCT02278588	-		Unknown	December 2016	United States, New York ... 展开 >> University at Buffalo Buffalo, New York, United States, 14214 收起 <<
NCT01187888	Progressive Supranuclear Palsy	Phase 3	Terminated(IMP used off label ... 展开 >>by phys. in pat. with PSP. Thus no more eligible patients were available for the study(pre-treatm.with Rasagiline=exclusion criterion) 收起 <<	-	Germany ... 展开 >> Department of Neurology and Palliative Care Klinikum der Universität München (Hospital of the University of Munich) München, Germany, 81377 收起 <<
NCT01385735	Parkinson Disease	Phase 4	Unknown	April 2013	Germany ... 展开 >> St. Josef Hospital Not yet recruiting Bochum, Nordrhein-Westfalen, Germany, 44791 Principal Investigator: Dirk Woitalla, MD Sub-Investigator: Irene Daum, Prof. 收起 <<
NCT01049984	-		Completed	-	-
NCT00955604	-		Completed	-	-
NCT01268891	Parkinson's Disease	Phase 3	Completed	-	-
NCT00696215	Parkinson's Disease	Phase 4	Unknown	October 2008	Turkey ... 展开 >> Marmara University Recruiting Istanbul, Turkey Contact: NESE TUNCER Raif Cakmur Recruiting Izmir, Turkey Contact: RAIF CAKMUR, PROF.DR 收起 <<
NCT01007630	Parkinson's Disease	Phase 4	Unknown	January 2014	United States, California ... 展开 >> The Parkinson's Institute Sunnyvale, California, United States, 94085 收起 <<
NCT00399477	Parkinson's Disease	Phase 4	Completed	-	-
NCT01497652	Parkinson's Disease	Phase 4	Completed	-	United States, District of Col... 展开 >>umbia Georgetown University Hospital Washington, District of Columbia, United States, 20007 收起 <<
NCT01532141	Parkinson Disease	Phase 1	Completed	-	France ... 展开 >> BIOTRIAL Rennes, France, F-35000 收起 <<
NCT01479530	Parkinson's Disease	Phase 3	Completed	-	China ... 展开 >> CN015 Beijing, China, 100034 CN008 Beijing, China, 100050 CN017 Beijing, China, 100050 CN001 Beijing, China, 100730 CN018 Beijing, China, 100730 CN011 Chengdu, China, 610041 CN003 Guangzhou, China, 510120 CN005 Guangzhou, China, 510180 CN004 Hangzhou, China, 310009 CN019 Qingyu Zhou, China, 510260 CN020 Qingyu Zhou, China, 510260 CN012 Shanghai, China, 200025 CN007 Shanghai, China, 200040 CN013 Shanghai, China, 200127 CN006 Suzhou, China, 215004 CN009 Wuhan, China, 430022 CN010 Xi'an, China, 710032 CN014 Zi'an, China, 710061 收起 <<
NCT01879241	Amyotrophic Lateral Sclerosis	Phase 2	Completed	-	Germany ... 展开 >> Department of Neurology, University of Ulm Ulm, Baden-Württemberg, Germany, 89081 Department of Neurology, Technische Universität München Muenchen, Bayern, Germany, D-81675 Department of Neurology, Universty of Regensburg Regensburg, Bayern, Germany, D-93053 Department of Neurology, University of Wuerzburg Wuerzburg, Bayern, Germany, 91054 Department of Neurology, Deutsche Klinik für Diagnostik Wiesbaden, Hessen, Germany, D-65191 Department of Neurology, University of Rostock Rostock, Mecklenburg-Vorpommern, Germany, D-18147 Department of Neurology, University of Goettingen Goettingen, Niedersachsen, Germany, D-37073 Department of Neurology, Medical School Hannover Hannover, Niedersachsen, Germany, 30625 Neurologische Universitätsklinik Bergmannsheil Bochum, Nordrhein-Westfalen, Germany, 44789 Department of Neurology, Universty of Muenster Muenster, Nordrhein-Westfalen, Germany, D-48149 Department of Neurology, Universty of Bonn Bonn, Nordrhrein-Westfalen, Germany, D-53105 Department of Neurology, University of Halle-Wittenberg Halle/Saale, Sachsen-Anhalt, Germany, 06097 Department of Neurology, TU Dresden Dresden, Sachsen, Germany, D-01307 Department of Neurology, University of Jena Jena, Thueringen, Germany, D-07747 Department of Neurology, Humboldt University Berlin, Germany, 13353 收起 <<
NCT01479530	-		Completed	-	-
NCT01723228	Parkinson's Disease	Phase 4	Completed	-	-
NCT01556165	Parkinson's Disease	Phase 3	Completed	-	China ... 展开 >> CN015 Beijing, China, 100034 CN001 Beijing, China, 100730 CN011 Chengdu, China, 610041 CN003 Guangzhou, China, 510120 CN005 Guangzhou, China, 510180 CN017 Guangzhou, China, 510260 CN004 Hangzhou, China, 310009 CN012 Shanghai, China, 200025 CN007 Shanghai, China, 200040 CN013 Shanghai, China, 200127 CN006 Suzhou, China, 215004 CN009 Wuhan, China, 430022 CN016 Wuhan, China, 430030 CN010 Xi'an, China, 710032 CN014 Xi'an, China, 710061 收起 <<
NCT01556165	-		Completed	-	-
NCT00755027	Parkinson's Disease	Phase 4	Completed	-	Spain ... 展开 >> Fundacio de Gestio Sanitaria de l'Hospital de la Santa Creu i Sant Pau Barcelona, Spain, 08025 收起 <<
NCT01232738	Amyotrophic Lateral Sclerosis ... 展开 >>(ALS) 收起 <<	Phase 2	Completed	-	United States, Arizona ... 展开 >> Phoenix Neurological Institute Phoenix, Arizona, United States, 85018 United States, California California Pacific Medical Center San Francisco, California, United States, 94118 United States, Iowa University of Iowa Iowa City, Iowa, United States, 52242 United States, Kansas University Of Kansas Medical Center Kansas City, Kansas, United States, 66160 United States, Minnesota University of Minnesota Minneapolis, Minnesota, United States, 55414 United States, Nebraska University of Nebraska Medical Center Omaha, Nebraska, United States, 68198 United States, Pennsylvania University of Pennsylvania Philadelphia, Pennsylvania, United States, 19104 United States, Tennessee University of Tennessee Memphis, Tennessee, United States, 38104 United States, Texas The Methodist Hospital System Houston, Texas, United States, 77030 Canada, Quebec McGill University Montreal, Quebec, Canada, H3A 2B4 收起 <<
NCT01723228	-		Completed	-	-
NCT01192503	Restless Legs Syndrome	Phase 2 Phase 3	Terminated(Slow enrollment)	-	United States, Florida ... 展开 >> Advent Research Pinellas Park, Florida, United States, 33781 United States, Georgia Medical College of Georgia Movements Disorders Program Augusta, Georgia, United States, 30912 United States, Illinois Northwestern University PD and Movement Disorders Center Chicago, Illinois, United States, 60611 United States, New Jersey Atlantic Neuroscience Institute Overlook Hospital Summit, New Jersey, United States, 07902 United States, New York SUNY- Buffalo Jacobs Neurological Institute Buffalo, New York, United States, 14203 United States, Ohio Cleveland Clinic Sleep Disorders Center Cleveland, Ohio, United States, 44195 United States, Pennsylvania University of Pennsylvania Sleep Center Philadelphia, Pennsylvania, United States, 19104 United States, Virginia Charlottesville Medical Research Charlottesville, Virginia, United States, 22911 收起 <<
NCT01268891	-		Completed	-	-
NCT02384512	-		Completed	-	-
NCT01532141	-		Completed	-	-
NCT01232738	-		Completed	-	-
NCT01652313	Parkinson's Disease	Phase 1	Completed	-	China ... 展开 >> CN001 Beijing, China 收起 <<
NCT01168596	-		Completed	-	-
NCT01786603	Amyotrophic Lateral Sclerosis ... 展开 >>(ALS) 收起 <<	Phase 2	Active, not recruiting	August 2017	United States, Arizona ... 展开 >> Phoenix Neurological Associates Phoenix, Arizona, United States, 85018 United States, California University of California - Irvine Irvine, California, United States, 92868 California Pacific Medical Center San Francisco, California, United States, 94115 United States, Kansas University of Kansas Medical Center Kansas City, Kansas, United States, 66160 United States, Missouri St. Louis University Saint Louis, Missouri, United States, 63104 United States, Nebraska University of Nebraska Omaha, Nebraska, United States, 68198 United States, New York Columbia University New York, New York, United States, 10032 United States, Oregon Oregon Health and Science University Portland, Oregon, United States, 97239 United States, Pennsylvania University of Pennsylvania Philadelphia, Pennsylvania, United States, 19107 United States, Texas UT Southwestern Medical Center Dallas, Texas, United States, 75390 收起 <<
NCT01736891	Parkinson´s Disease	Phase 3	Completed	-	China ... 展开 >> CN002 Chengdu, China, 610041 CN005 Chenzhou, China, 423000 CN007 Chongqing, China, 404000 CN003 Guilin, China, 541001 CN004 Lanzhou, China, 730050 CN006 Luzhou, China, 646000 CN008 Nanjing, China, 210029 CN001 Xi'an, China, 710032 收起 <<
NCT01178047	Parkinson's Disease	Phase 4	Terminated(payments stopped by... 展开 >> grant provider) 收起 <<	-	Switzerland ... 展开 >> University Hospital, Neurology Zurich, ZH, Switzerland, CH-8091 Neurocentro, Lugano Lugano, Switzerland 收起 <<
NCT01442610	Sleep Disturbances ... 展开 >> Parkinsons's Disease 收起 <<	Phase 4	Completed	-	Germany ... 展开 >> Dresden University of Technology, Dept. of Neurology Dresden, Germany, 01307 收起 <<
NCT00203177	Parkinson's Disease	Phase 3	Completed	-	United States, California ... 展开 >> Margolin Brain Institute Fresno, California, United States, 93720 United States, Georgia Emory University Atlanta, Georgia, United States, 30329 United States, Illinois Rush - Presbyterian St. Luke's Medical Center Chicago, Illinois, United States, 60612 United States, Nebraska Creighton University Omaha, Nebraska, United States, 68131 United States, New York Long Island Jewish Medical Center New Hyde Park, New York, United States, 11040 University of Rochester Rochester, New York, United States, 14642 United States, Pennsylvania Pennsylvania Hospital Philadelphia, Pennsylvania, United States, 19107 Canada, Quebec CHUM-Hotel-Dieu Montreal, Quebec, Canada, H2w1T8 收起 <<
NCT00977665	Multiple System Atrophy	Phase 2	Completed	-	-
NCT00936676	-		Completed	-	-
NCT01032486	-		Completed	-	-
NCT00977665	-		Completed	-	-
NCT03727139	-		Recruiting	October 31, 2021	Japan ... 展开 >> Takeda Selected Site Recruiting Tokyo, Japan 收起 <<
NCT01168596	Parkinson's Disease	Phase 4	Completed	-	United States, Colorado ... 展开 >> University of Colorado Anschutz outpatient Pavilion Aurora, Colorado, United States, 80045 United States, Florida Shands and University of Florida Medical Plaza Gainesville, Florida, United States, 32610 United States, Ohio Cleveland Clinic Center for Neurological Restoration Cleveland, Ohio, United States, 44195 收起 <<
NCT00203164	Parkinson's Disease	Phase 3	Completed	-	United States, California ... 展开 >> Margolin Brain Institute Fresno, California, United States, 93720 United States, Illinois Rush - Presbyterian St. Luke's Medical Center Chicago, Illinois, United States, 60612 United States, Nebraska Creighton University Omaha, Nebraska, United States, 68131 United States, New York Long Island Jewish Medical Center New Hyde Park, New York, United States, 11040 University of Rochester Rochester, New York, United States, 14642 United States, Pennsylvania Pennsylvania Hospital Philadelphia, Pennsylvania, United States, 19107 收起 <<
NCT01879748	Parkinson's Disease	Phase 1	Completed	-	United States, California ... 展开 >> Teva Investigational Site 10738 Glendale, California, United States 收起 <<

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