Cas No.: | 1161233-85-7 |
Chemical Name: | BTZ043 |
Synonyms: | BTZ043;2-[(3S)-3-methyl-1,4-dioxa-8-azaspiro[4.5]decan-8-yl]-8-nitro-6-(trifluoromethyl)-1,3-benzothiazin-4-one;BTZ-043;2-[(2S)-2-Methyl-1,4-dioxa-8-azaspiro[4.5]decan-8-yl]-8-nitro-6-trifluoromethyl-4H-1,3-benzothiazin-4-one;BTZ 043;G55ZH52P57;MMV676603;(S)-2-(2-methyl-1,4-dioxa-8-azaspiro[4.5]decan-8-yl)-8-nitro-6-(trifluoromethyl)-4H-benzo[e][1,3]thiazin-4-one;S1097_Selleck;PBTZ 169;BCPP000312;SB22928;BCP9000457;BTZ 10526043;4H-1,3-Benzothiazin-4-one, 2-[(2S)-2-methyl-1,4-dioxa-8-azaspiro[4.5]dec-8-yl]-8-nitro-6;Unii-G55ZH52P57;Q27278777;4H-1,3-Benzothiazin-4-one, 2-[(2S)-2-methyl-1,4-dioxa-8-azaspiro[4.5]dec-8-yl]-8-nitro-6-(triflu |
SMILES: | O=C1N=C(N(CC2)CCC32OC[C@H](C)O3)SC4=C([N+]([O-])=O)C=C(C(F)(F)F)C=C14 |
Formula: | C17H16F3N3O5S |
M.Wt: | 431.39 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | BTZ043 is an inhibitor of decaprenyl-phosphoribose-epimerase (DprE1), with MICs of of 2.3 nM and 9.2 nM for M. tuberculosis H37Rv and Mycobacterium smegmatis, respectively. |
In Vivo: | Four weeks of treatment with BTZ043 reduces the bacterial burden in the lungs and spleens by 1 and 2 logs, respectively, at the concentrations used. Additional results suggest that BTZ043 efficacy is time-rather than dose-dependent. Acute (5 g/kg) and chronic (25 and 250 mg/kg) toxicology studies in uninfected mice show that, even at the highest dose tested, there are no adverse anatomical, behavioral, or physiological effects after one month[2]. |
In Vitro: | The MIC of BTZ043 against M. tuberculosis H37Rv and Mycobacterium smegmatis are 1 ng/mL (2.3 nM) and 4 ng/mL (9.2 nM), respectively[2]. The in vitro activity of BTZ043 against 30 Nocardia brasiliensis isolates is also tested. The MIC50 and MIC90 values for BTZ043 are 0.125 and 0.25 μg/mL. The MIC for N. carnea ATCC 6847 is 0.003μg/mL, for N. transvalensis ATCC 6865 is 0.003μg/mL, for N. brasiliensis NCTC10300 is 0.03 μg/mL, and for N. brasiliensis HUJEG-1 is 0.125μg/mL. The MIC value for M. tuberculosis H37Rv is 0.000976 μg/mL. The MIC value of BTZ-043 is >64 μg/mL for Escherichia coli ATCC 25922 and S. aureus ATCC 29213[3]. |