您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
位置:首页 > 产品库 > PBTZ169
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
PBTZ169
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
PBTZ169图片
CAS NO:1377239-83-2
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
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 SMILESO=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 tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation 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.