位置:首页 > 产品库 > NITD-349
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:
 
NITD-349
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。
NITD-349图片
CAS NO:1473450-62-2
包装与价格:
包装价格(元)
2 mg询价
5 mg询价
10 mg询价
50 mg询价
100 mg询价
200 mg询价
1 mL*10 mM(in DMSO)询价

NITD-349 是MmpL3的抑制剂,它对毒性结核分枝杆菌 H37Rv 显示出高效的抗分枝杆菌活性,MIC50 为 23 nM。

产品描述

NITD-349 is an inhibitor of MmpL3. It shows highly potent anti-mycobacterial activity with MIC50 of 23 nM against virulent Mycobacterium tuberculosis H37Rv.

体外活性

NITD-304 and NITD-349, showed potent activity against both drug-sensitive and multidrug-resistant clinical isolates of Mtb.?Promising pharmacokinetic profiles of both compounds after oral dosing in several species enabled further evaluation for efficacy and safety.?NITD-304 and NITD-349 were efficacious in treating both acute and chronic Mtb infections in mouse efficacy models.?Furthermore, dosing of NITD-304 and NITD-349 for 2 weeks in exploratory rat toxicology studies revealed a promising safety margin.?Finally, neither compound inhibited the activity of major cytochrome P-450 enzymes or the hERG (human ether-a-go-go related gene) channel[1].

体内活性

In the acute murine efficacy model, treatment of mice with NITD-349 at doses of 12.5 and 50 mg/kg resulted in 0.9- and 3.4-log CFU reduction in lung tissue.?In an established infection mouse model, after 2 weeks of treatment, the efficacy of NITD-349 is comparable to the first-line TB drug rifampicin and is better than ethambutol.?Four weeks of treatment at 100 mg/kg with NITD-349 results in 2.38-log CFU reductions[1].

Cas No.

1473450-62-2

分子式

C17H20F2N2O

分子量

306.35

别名

NITD-349

储存和溶解度

DMSO:310 mg/mL (1011.91 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years
 
 
维奥蛋白资源库 - 中文蛋白资源 CopyRight © 2010-2024