BTZ043 (BTZ038, BTZ044) is a decaprenylphosphoryl-b-D-ribose 2-epimerase inhibitor. BTZ043 (BTZ038, BTZ044) is an enzyme which produces the cell wall of the pathogenic bacterium Mycobacterium tuberculosis. The MIC of BTZ043 racemate against M. tuberculosis H37Rv and Mycobacterium smegmatis were 1 ng/ml and 4 ng/ml, respectively.
Cell Experiment | |
---|---|
Cell lines | macrophages infected with GFP-labeled M. tuberculosis |
Preparation method | Intracellular activity of BTZ. Raw 264.7 macrophages (ATCC # TIB-71) (1.5 x 108 cells) were infected with H37Rv-GFP at an MOI of 1:1 in 300 ml of RPMI 1640 (Gibco) with 10% heat-inactivated fetal calf serum (Gibco) for 2 h at 37 °C with shaking (100 rpm). For each compound, a series of 16 two-fold dilutions in quadruplicate was tested. Infected cells were then incubated in the presence of the compound for 5 days at 37 °C, 5% CO2. Then, macrophages were stained with SYTO 60 (Invitrogen, S11342) followed by plate sealing and image acquisition. Confocal images were recorded on an automated fluorescent confocal microscope OperaTM (PerkinElmer) using a 20X-water objective (NA 0.70). Mycobacteria-GFP are detected using a 488-nm laser coupled with a 535/50 nm detection filter (green channel, GFP excitation) and cells labeled with Syto 60 are identified with 635-nm laser coupled with a 690/40 nm detection filter (red channel, Syto 60 excitation). |
Concentrations | 0~1 μ M |
Incubation time | 5 days |
Animal Experiment | |
---|---|
Animal models | M. tuberculosis H37Rv infected BALB/c mice chronical model |
Formulation | carboxymethyl cellulose formulation (0.25%) |
Dosages | 37.5 or 300 mg/kg once daily, six times/week for four weeks |
Administration | gavage |
Molecular Weight | 431.39 |
Formula | C17H16F3N3O5S |
CAS Number | 957217-65-1 |
Solubility (25°C) | DMSO |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
Related Anti-infection Products |
---|
Acetylalkannin
Acetylalkannin (Alkannin acetate) is an isohexenylnaphthazarin pigment isolated from Arnebia euchroma with antimicrobial and cytotoxic activities. |
Chimeric Rabies Virus Glycoprotein Fragment (RVG-9R)
Chimeric Rabies Virus Glycoprotein Fragment (RVG-9R), a chimeric peptide consisting of 29 amino acids, is synthesized by adding nona-arginine motif to the carboxy terminus of RVG (rabies virus glycoprotein). |
LCMV GP (61-80)
LCMV GP (61-80) is a peptide fragment derived from lymphocytic choriomeningitis virus (LCMV) glycoprotein (GP), and corresponds to amino acids 61-80. |
Histone H4 (2-21)
Histone H4 (2-21) is the core histones associated with chromatinization of herpes simplex virus 1 (HSV-1) genomes. |
TAT (48-57)
TAT (48-57) is a cell-permeable peptide, derived from HIV-1 transactivator of transcription (Tat) protein residue 48-57. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.