TMC-207

한글명:TMC-207

카스 번호843663-66-1

상품명:TMC-207

CBNumberCB12473722

분자식C32H31BrN2O2

포뮬러 무게555.5

MOL 파일843663-66-1.mol

화학적 성질

녹는점	104 °C
끓는 점	702.7±60.0 °C(Predicted)
밀도	1.322±0.06 g/cm3(Predicted)
저장 조건	Room temperature
용해도	DMSO에 용해됨(10mg/ml)
물리적 상태	고체
물리적 상태	단단한 모양
산도 계수 (pKa)	13.05±0.29(Predicted)
색상	하얀색
안정성	제공된 대로 구매일로부터 1년 동안 안정적입니다. DMSO의 솔루션은 -20°C에서 최대 1개월 동안 보관할 수 있습니다.
CAS 데이터베이스	843663-66-1

위험 및 안전 성명

HS 번호

2933499090

유해 물질 데이터

843663-66-1(Hazardous Substances Data)

NFPA 704:

	0
2		0

그림문자(GHS)

TMC-207 화학적 특성, 용도, 생산

개요
In December 2012, the US FDA approved bedaquiline as part of combination therapy for the treatment of multi-drug resistant tuberculosis (MDRTB). Bedaquiline is the first drug approved for MDR-TB and is the first approval from a new class of antituberculosis agents in the past 40 years. Due to the high unmetmedical need for treating MDR-TB, the FDA granted bedaquiline accelerated approval based on Phase II results, providing patients access to the drug while additional clinical studies are carried out. Bedaquiline (also known as TMC207 and R207910) is a diarylquinoline that was discovered from a high-throughput, whole-cell screening strategy with Mycobacterium smegmatis used as a surrogate for M. tuberculosis. Bedaquiline is a single enantiomer of an initial screening hit. Bedaquiline has potent and selective activity against mycobacteria, and is active against both drug-sensitive and drug-resistant M. tuberculosis. The mechanism of action of bedaquiline is unique amongst anti-TB drugs and involves inhibition of mycobacterial ATP synthase; it is not active against human ATP synthase. Bedaquiline has in vivo activity in numerous preclinical models of TB infection, alone and in combination with other anti-TB agents, and has bactericidal activity in established TB infection models. Bedaquiline is synthesized in five steps from 3-phenylpropionic acid and para-bromoaniline. Following amide formation, treatment with POCl₃ and DMF under Vilsmeier–Hack conditions gave a 2-chloroquinoline product. Treatment with sodium methoxide, followed by condensation with 3-(dimethylamino)-1-(naphthalen-1-yl)propan-1-one, and separation of isomers gave bedaquiline.
용도
(αS,βR)-Bedaquiline is a diarylquinoline derivative that acts as a mycobacterial inhibitor. Bedaquiline shows promise as potential drug in the treatment of tuberculosis.

TMC-207 준비 용품 및 원자재

TMC-207 공급 업체

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