PBTZ169

An antibiotic with antimycobacterial activity

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库存: 现货

可选规格

包装

价格

促销价

数量
5mg

￥987.00

790.00

- +
10mg

￥1637.00

1310.00

- +
50mg

￥5325.00

4260.00

- +
100mg

￥7775.00

6220.00

- +

已选 0 种 0 瓶

金额: ￥0.00

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Background

PBTZ169 is a new drug candicate that inhibits decaprenylphosphoryl-β-d-ribose 2′-oxidase (DprE1), more efficiently than BTZ043target: DprE1In vitro: PBTZ169, inhibit decaprenylphosphoryl-β-d-ribose 2′-oxidase (DprE1) and display nanomolar bactericidal activity against Mycobacterium tuberculosis in vitro. [1]In vivo: 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 ug/mL, respectively. The MIC for PBTZ169 for N. brasiliensis HUJEG-1 was 0.0037 ug/mL.[2] PBTZ169 has improved potency, safety and efficacy in zebrafish and mouse models of tuberculosis (TB). [3]

参考文献:
[1]. [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]. [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.
[3]. [3] Makarov V et al. Towards a new combination therapy for tuberculosis with next generation benzothiazinones.EMBO Mol Med. 2014 Mar;6(3):372-83.