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SML4247

TMC207 fumarate

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

Synonym(s):

(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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About This Item

Empirical Formula (Hill Notation):
C32H31BrN2O2· C4H4O4
CAS Number:
845533-86-0
Molecular Weight:
671.58
MDL number:
MFCD28167761
NACRES:
NA.21
Assay:
≥98% (HPLC)
Form:
powder
Storage condition:
desiccated
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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

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

pictograms

Environment
GHS09

signalword

Warning

hcodes

H410

Hazard Classifications

Aquatic Chronic 1

Storage Class

11 - Combustible Solids

flash_point_f

Not applicable

flash_point_c

Not applicable

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