SML4247
TMC207 fumarate
≥98% (HPLC)
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:
Molecular Weight:
671.58
MDL number:
UNSPSC Code:
12352200
Quality Level
assay
≥98% (HPLC)
form
powder
storage condition
desiccated
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
-10 to -25°C
Biochem/physiol Actions
TMC207 (Bedaquiline) fumarate′s enhanced solubility ensures reliable oral delivery, powering its potent and selective ATP synthase inhibition for bactericidal action against Mycobacterium tuberculosis.
TMC207 (Bedaquiline) fumarate, the salt form of the antitubercular drug bedaquiline, 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.
TMC207 (Bedaquiline) fumarate, the salt form of the antitubercular drug bedaquiline, 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.
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Hygroscopic Store with dessicant
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