S83048 |
PBTZ169 |
源叶(MedMol) | 98% |
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- 产品描述: PBTZ169 inhibits decaprenylphosphoryl-β-d-ribose 2′-oxidase (DprE1), more efficiently than BTZ043.
- 靶点: Antibacterial;DprE1;Antibacterial; DprE1
- 体外研究:
PBTZ169, inhibit decaprenylphosphoryl-β-d-ribose 2′-oxidase (DprE1) and display nanomolar bactericidal activity against Mycobacterium tuberculosis in vitro.
- 体内研究:
PBTZ169 can be suspend in 0.25% hydroxy-propylmethyl-cellulose. The administertration for PBTZ169 is 100 mg/kg by gavage. The MIC50 and MIC90 values were 0.0075 and 0.030 μg/mL, respectively. The MIC for PBTZ169 for N. brasiliensis HUJEG-1 was 0.0037 μg/mL. PBTZ169 has improved potency, safety and efficacy in zebrafish and mouse models of tuberculosis (TB).
- 参考文献:
1. Makarov V,et al. The 8-Pyrrole-Benzothiazinones Are Noncovalent Inhibitors of DprE1 from Mycobacterium tuberculosis. Antimicrob Agents Chemother. 2015 Aug;59(8):4446-52. 2. González-Martínez NA,et al. In Vivo Activity of the Benzothiazinones PBTZ169 and BTZ043 against Nocardia brasiliensis. PLoS Negl Trop Dis. 2015 Oct 16;9(10):e0004022.
- 溶解性: Soluble in DMSO
- 保存条件: -20℃
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 2.191 ml 10.953 ml 21.907 ml 5 mM 0.438 ml 2.191 ml 4.381 ml 10 mM 0.219 ml 1.095 ml 2.191 ml 50 mM 0.044 ml 0.219 ml 0.438 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)