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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C17H16F3N3O5S |
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分子量 | 431.39 | CAS No. | 957217-65-1 | |
Solubility (25°C)* | 体外 | DMSO | 22 mg/mL (50.99 mM) | |
Ethanol | 3 mg/mL (6.95 mM) | |||
Water | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
製品説明 | BTZ043 racemate is a decaprenylphosphoryl-β-D-ribose 2'-epimerase (DprE1) inhibitor acting as a new antimycobacterial agent that kill Mycobacterium tuberculosis. |
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in vitro | By targeting decaprenylphosphoryl-β-D-ribose 2'-epimerase, BTZ043 abolishes the formation of decaprenylphosphoryl arabinose, leading to cell lysis and death of Mycobacterium tuberculosis. BTZ043 displays similar activity against all clinical isolates of M. tuberculosis, including multidrug-resistant and extensively drug-resistant strains. BTZ043 displays significant activity against M. tuberculosis H37Rv and Mycobacterium smegmatis with MIC of 1 ng/mL (2.3 nM) and 4 ng/mL (9.2 nM), respectively, which is more potent than those of the existing tuberculosis (TB) drugs isoniazid (INH) and ethambutol (EMB) with MIC of 0.02-0.2 μg/mL and 1-5 μg/mL, respectively. BTZ043 is less effective in two different model systems (auxotrophy and starvation) involving metabolically inert M. tuberculosis, indicating that BTZ043 blocks a step in active metabolism similar to isoniazid (INH). BTZ043 treatment in M. smegmatis cells decreases the growth rate rapidly followed by a swelling of the poles and lysis of the cells after a few hours, which is similar but delayed in M. tuberculosis. [1] BTZ043 (1/4 MIC 0.375 ng/mL) in combination with TMC207 (1/4 MIC 20 ng/mL) has a stronger cidal effect on M. tuberculosis but not BTZ-resistant M. tuberculosis mutant than TMC207 alone at a concentration of 80 ng/mL. [2] |
in vivo | In a mouse model of chronic tuberculosis, administration of BTZ043 at 37.5 mg/kg or 300 mg/kg for 4 weeks reduces the bacterial burden in the lungs and spleens by 1 and 2 logs, respectively. [1] |
特徴 | Greater activity against M. tuberculosis than EMB. |
動物実験 | 動物モデル | BALB/c mice infected with a low bacillary load (~200 CFU) of M. tuberculosis H37Rv via aerosol |
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投薬量 | 37.5 mg/kg, or 300 mg/kg | |
投与方法 | Oral gavage once daily |
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Spray-dried lactose-leucine microparticles for pulmonary delivery of antimycobacterial nanopharmaceuticals [ Drug Deliv Transl Res, 2021, 11(4):1766-1778] | PubMed: 34101127 |
Optimization of Hydantoins as Potent Antimycobacterial Decaprenylphosphoryl-β-d-Ribose Oxidase (DprE1) Inhibitors [ J Med Chem, 2020, 28;63(10):5367-5386] | PubMed: 32342688 |
Oncolytic immunotherapy and bortezomib synergy improves survival of refractory multiple myeloma in a preclinical model [ Blood Adv, 2019, 3(5):797-812] | PubMed: 30850386 |
Loperamide overcomes the resistance of colon cancer cells to bortezomib by inducing CHOP-mediated paraptosis-like cell death [ Biochem Pharmacol, 2019, 162:41-54] | PubMed: 30529689 |
N-methylation of a bactericidal compound as a resistance mechanism in Mycobacterium tuberculosis. [ Proc Natl Acad Sci U S A, 2016, 113(31):E4523-30] | PubMed: 27432954 |
Whole Cell Target Engagement Identifies Novel Inhibitors of Mycobacterium tuberculosis Decaprenylphosphoryl-β-d-ribose Oxidase. [ ACS Infect Dis, 2015, 1(12):615-26] | PubMed: 27623058 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。