BTZ043 racemate|2mg|K1374-上海高创化学科技有限公司

BTZ043 racemate

参考价：¥1298

供货周期：

一周

品牌：

规格：

2mg

货号：

K1374

CAS号：

957217-65-1

SKU:K1374		M. Wt:431.39
Formula:C17H16F3N3O5S		Solubility:No
Purity:>99%		Storage:2 years at -20 degrees centigrade
CAS No.:957217-65-1		Synonyms:BTZ038, BTZ044
Chemical NameN/A

Description	BTZ043 racemate
Targets	Mycobacterium tuberculosis
IC50	N/A
In vitro	BTZ043, is a candidate for inclusion in combination therapies for both drug-sensitive and extensively drug-resistant TB. The MIC of BTZ043 against M. tuberculosis H37Rv and Mycobacterium smegmatis were 1 ng/ml (2.3 nM) and 4 ng/ml (9.2 nM), respectively. BTZ043 displays similar activity against all clinical isolates of M. tuberculosis that were tested, including multidrug-resistant and extensively drug-resistant strains. BTZ043 is bactericidal, reducing viability in vitro by more than 1000-fold in under 72 hours, which is comparable to the killing effect seen with INH.[1] BTZ043 acts synergistically with TMC207, with a fractional inhibitory concentration index of 0.5. TMC207 at a quarter of the MIC (20 ng/ml) used in combination with BTZ043 (1/4 MIC, 0.375 ng/ml) had a stronger bactericidal effect on M. tuberculosis than TMC207 alone at a concentration of 80 ng/ml. The sub-MICs of BTZ043 weaken the bacterial cell wall and allow improved penetration of TMC207 to its target.[2]
In vivo	In two different model systems (auxotrophy and starvation) involving metabolically inert M. tuberculosis, BTZ043 was less effective, which implies that it blocks a step in active metabolism, similar to INH.[1]
Clinical Trials	N/A
Features	N/A

Description

BTZ043 racemate

Targets

Mycobacterium tuberculosis

IC50

N/A

In vitro

BTZ043, is a candidate for inclusion in combination therapies for both drug-sensitive and extensively drug-resistant TB. The MIC of BTZ043 against M. tuberculosis H37Rv and Mycobacterium smegmatis were 1 ng/ml (2.3 nM) and 4 ng/ml (9.2 nM), respectively. BTZ043 displays similar activity against all clinical isolates of M. tuberculosis that were tested, including multidrug-resistant and extensively drug-resistant strains. BTZ043 is bactericidal, reducing viability in vitro by more than 1000-fold in under 72 hours, which is comparable to the killing effect seen with INH.[1] BTZ043 acts synergistically with TMC207, with a fractional inhibitory concentration index of 0.5. TMC207 at a quarter of the MIC (20 ng/ml) used in combination with BTZ043 (1/4 MIC, 0.375 ng/ml) had a stronger bactericidal effect on M. tuberculosis than TMC207 alone at a concentration of 80 ng/ml. The sub-MICs of BTZ043 weaken the bacterial cell wall and allow improved penetration of TMC207 to its target.[2]

In vivo

In two different model systems (auxotrophy and starvation) involving metabolically inert M. tuberculosis, BTZ043 was less effective, which implies that it blocks a step in active metabolism, similar to INH.[1]

Clinical Trials

N/A

Features

N/A