미라베그론

미라베그론 속성

미라베그론 C화학적 특성, 용도, 생산

개요

Betanis (Mirabegron) was approved in July 2011 by the Japanese Ministry of Health, Labour, and Welfare for the treatment of urgency, urinary frequency, and urinary urge urinary incontinence associated with overactive bladder (OAB). Mirabegron is synthesized by coupling 4-nitrophenethyl amine to (R)-2-hydroxy-2-phenylacetic acid. The resulting amide is reduced to an amine. The nitro group is then reduced and the resulting aniline is coupled to 2-(2-aminothiazol-4-yl) acetic acid to give mirabegron. Mirabegron has an EC₅₀ of 22 nM (intrinsic activity=0.8) for β3-AR with no detectable activity for β1- andβ2-AR (EC₅₀>10,000 nM). In an anesthetized rat rhythmic bladder contraction model in which bladder contractions are induced by saline, mirabegron at 3 mg/kg iv decreased the frequency of rhythmic bladder contraction without suppressing contraction amplitude. These data suggest that the activation of β3-AR increases bladder capacity without influencing the frequency of bladder contraction.

화학적 성질

White to Off-White Solid

용도

Potent bladder relaxant and reagent for diabetes remedy.;Labeled Mirabegron, intended for use as an internal standard for the quantification of Mirabegron by GC- or LC-mass spectrometry.

정의

ChEBI: A monocarboxylic acid amide obtained by formal condensation of the carboxy group of 2-amino-1,3-thiazol-4-ylacetic acid with the anilino group of (1R)-2-{[2-(4-aminophenyl)ethyl]amino}-1-phenylethanol. Used for the treatment of overactive ladder syndrome.

Clinical Use

Mirabegron is an orally active β3-adrenoceptor agonist currently in development by Astellas Pharma for the treatment of overactive bladder (OAB). The drug is a nanomolar EC50 antagonist against human β3-AR biochemical assays with good selectivity over b1- and β2-ARs. Mirabegron demonstrates a novel mechanism by targeting the β3-AR for bladder relaxation to help manage OAB symptoms such as increased urinary urgency and frequency and urgency incontinence. However, mirabegron is a cytochrome P450 2D6 inhibitor, and it raises a concern for drug–drug interaction with concomitant administration of other cytochrome P450 2D6 substrates.

미라베그론 준비 용품 및 원자재

원자재

준비 용품

미라베그론 공급 업체

공급자	전화	이메일	국가	제품 수	이점
Anhui Dexinjia Biopharm Co., Ltd	+86-531-82375887 +86-15064153060	sales01@ahdxj.com	China	293	58
Beijing Mesochem Technology Co.,Ltd	+8613651027935	rachel@mesochem.com	China	191	58
Siyang Liaoning Biochemical Products Co. Ltd	+86-15221114306; +8615221114306	2594582574@qq.com	China	574	58
Shenzhen Excellent Biomedical Technology Co.,Ltd.	+86-0755-26050679 +86-15915472436	sale@ex-biotech.cn	China	1031	58
shandong perfect biotechnology co.ltd	+86-53169958659; +8618596095638	sales@sdperfect.com	China	294	58
Henan Tengmao Chemical Technology Co. LTD	+8615238638457	salesvip2@hntmhg.com	China	415	58
Anhui Zhongda Biotechnology Co., Ltd	+8619956560829	justine@zhongda-biotech.com	China	300	58
Shaanxi TNJONE Pharmaceutical Co., Ltd	+8618740459177	sarah@tnjone.com	China	1141	58
Capot Chemical Co.,Ltd.	571-85586718 +8613336195806	sales@capotchem.com	China	29797	60
Beijing Cooperate Pharmaceutical Co.,Ltd	010-60279497	sales01@cooperate-pharm.com	CHINA	1811	55

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