|PBTZ169 目录号 GC19276|
Sample solution is provided at 25 µL, 10mM.
|Cas No.||1377239-83-2||SDF||Download SDF|
|溶解度||DMSO : 6.4 mg/mL (14.02 mM; Need ultrasonic)||储存条件||Store at -20°C|
|General tips||For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.|
|Shipping Condition||Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
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. 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. PBTZ169 has improved potency, safety and efficacy in zebrafish and mouse models of tuberculosis (TB). 
.  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.
.  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.
.  Makarov V et al. Towards a new combination therapy for tuberculosis with next generation benzothiazinones.EMBO Mol Med. 2014 Mar;6(3):372-83.