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SML4247

TMC207 fumarate

Name: TMC207 fumarate
Brand: SIGMA

≥98% (HPLC), powder, mycobacterial ATP synthase inhibitor

别名:

(1R, 2S)-1-(6-Bromo-2methoxy-3-quinolinyl)-4-(dimethylamino)-2-(1-naphthalenyl)-1-phenyl-2-butanol, fumaric acid (1:1), Bedaquiline fumarate, R 207910 fumarate, R-207910 fumarate, R207910 fumarate

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关于此项目

经验公式（希尔记法）:

C₃₂H₃₁BrN₂O₂· C₄H₄O₄

化学文摘社编号:

845533-86-0

分子量:

671.58

MDL number:

MFCD28167761

NACRES:

NA.21

UNSPSC Code:

12352200

Assay:

≥98% (HPLC)

Form:

powder

Storage condition:

desiccated

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属性

Quality Segment

100

assay

≥98% (HPLC)

form

powder

storage condition

desiccated

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

-10 to -25°C

说明

General description

TMC207 (Bedaquiline) is an diarylquionline antimycobacterial agent. TMC207 fumarate is the salt form of the antitubercular drug bedaquiline.

Application

TMC207 fumarate may be used to study the pharmacodynamic activity of Bedaquiline loaded fucosylated/nonfucosylated liposomes (BDQ-Lipofuc/BDQ-Lipo) in a mouse model of Mycobacterium tuberculosis infection.

Biochem/physiol Actions

TMC207 (Bedaquiline) fumarate potently inhibits Mycobacterium tuberculosis (MIC50 ~0.03 µg/mL) by selectively targeting the c-subunit of its ATP synthase, thereby disrupting cellular energy and leading to cell death, while exhibiting minimal interaction with human ATP synthase (selectivity index >20,000). This specific salt formulation provides enhanced aqueous solubility and dissolution, contributing to favorable ADME properties, improved and more consistent oral bioavailability, and a very long terminal elimination half-life (approximately 5.5 months), ensuring sustained and predictable exposure at the site of infection.

Disclaimer

Hygroscopic Store with dessicant

象形图

GHS09

警示词

Warning

危险代码

H410

预防性声明

P273 - P391 - P501

Hazard Classifications

Aquatic Chronic 1

存储类别

11 - Combustible Solids

闪点 (F)

Not applicable

闪点 (°C)