PBTZ169 (PBTZ169) 是一种杀菌苯并噻嗪酮和有效的 DprE1 (decaprenylphosphoryl-⋲-d-ribose 2′-oxidase) 抑制剂。
| Cas No. | 1377239-83-2 |
| 别名 | PBTZ169 |
| Canonical SMILES | O=C1C2=CC(C(F)(F)F)=CC([N+]([O-])=O)=C2SC(N3CCN(CC4CCCCC4)CC3)=N1 |
| 分子式 | C20H23F3N4O3S |
| 分子量 | 456.48 |
| 溶解度 | DMSO : 6.4 mg/mL (14.02 mM) |
| 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 |
| 产品描述 | 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] References:
[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. |
