SML4247

TMC207 fumarate

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

• Synonym(e): (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
• Empirische Formel (Hill-System): C₃₂H₃₁BrN₂O₂· C₄H₄O₄
• CAS-Nummer: 845533-86-0
• Molekulargewicht: 671.58
• MDL number: MFCD28167761
• NACRES: NA.21
• UNSPSC Code: 12352200
• Assay: ≥98% (HPLC)
• Form: powder
• Storage condition: desiccated

Eigenschaften

• 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

Beschreibung

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

Sicherheitshinweise

• Piktogramme: GHS09
• Signalwort: Warning
• Gefahrencodes: H410
• Sicherheitshinweise: P273 - P391 - P501
• Hazard Classifications: Aquatic Chronic 1
• Lagerklasse: 11 - Combustible Solids
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable