[CAS NO. 843663-66-1] Bedaquiline

Name: Bedaquiline
Brand: Arctom Scientific
SKU: SLK-S5623

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PRODUCTS SPECIFICATIONS [843663-66-1]

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Catalog

SLK-S5623

Brand

Selleck

CAS

843663-66-1

DESCRIPTION [843663-66-1]

Overview

MDL	MFCD14635354
Molecular Weight	555.50
Molecular Formula	C32H31BrN2O2
SMILES	[C@]([C@@H](C=1C(OC)=NC2=C(C1)C=C(Br)C=C2)C3=CC=CC=C3)(CCN(C)C)(O)C=4C5=C(C=CC4)C=CC=C5

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	1.8002 mL	9.0009 mL	18.0018 mL
5 mM	0.3600 mL	1.8002 mL	3.6004 mL
10 mM	0.1800 mL	0.9001 mL	1.8002 mL
50 mM	0.0360 mL	0.1800 mL	0.3600 mL

Description

Bedaquiline (TMC-207, R207910), a diarylquinoline, binds to subunit c of and inhibits its activity. It is highly selective for mycobacterial ATP synthase enzyme compared to homologous eukaryotic enzyme (Selectivity Index >20 000).

Targets

mycobacterial ATP synthase ^[1]

In vitro

Bedaquiline targets against Mycobacterial ATP synthase complex. Bedaquiline has anti-cancer activity, directed against Cancer Stem-like Cells (CSCs). Bedaquiline treatment of MCF7 breast cancer cells inhibits mitochondrial oxygen-consumption, as well as glycolysis, but induces oxidative stress. Bedaquiline reduces mitochondrial membrane potential, with a significant rise in ROS levels. It specifically inhibits mitochondrial respiration in cancer cells, while enhancing mitochondrial function in normal cells. Bedaquiline dramatically inhibits oxygen consumption and ATP production in the low micromolar range. In addition, bedaquiline treatment also reduced aerobic glycolysis.

In vivo

Bedaquiline follows triphasic elimination and characterized by an outstandingly long terminal half-life, around 173 h in humans.

References

[1] Mageshwaran Lakshmanan, et al. J Young Pharm. 2013, 5(4): 112–115.
[2] Fiorillo M, et al. Aging (Albany NY). 2016, 8(8):1593-607.

Synonyms

3-Quinolineethanol, 6-bromo-α-[2-(dimethylamino)ethyl]-2-methoxy-α-1-naphthalenyl-β-phenyl-, (αS,βR)-

(αS,βR)-6-Bromo-α-[2-(dimethylamino)ethyl]-2-methoxy-α-1-naphthalenyl-β-phenyl-3-quinolineethanol

R 207910

TMC 207

Bedaquiline

Sirturo