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DprE1-IN-1
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。
DprE1-IN-1图片
CAS NO:1494675-86-3
包装与价格:
包装价格(元)
2mg电议
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
DprE1-IN-1 是一种有效的非共价 DprE1 抑制剂。
Cas No.1494675-86-3
别名N-(2-羟基乙基)-1-[(6-甲氧基-5-甲基嘧啶-4-基)甲基]-6-甲基-1H-吡咯并[3,2-B]吡啶-3-甲酰胺
Canonical SMILESO=C(C1=CN(CC2=NC=NC(OC)=C2C)C3=CC(C)=CN=C31)NCCO
分子式C18H21N5O3
分子量355.39
溶解度DMSO : 11 mg/mL (30.95 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

DprE1-IN-1 is a potent DprE1 inhibitor, with ic50 of 10 nM, also inhibits PDE6, with IC50 of 6 uM.IC50 value: 10 nM [1]Target: DprE1in vitro: DprE1-IN-1 demonstrats efficacy in a rodent model of tuberculosis, making it promising for further development.[1]in vivo: The pharmacokinetic profile of DprE1-IN-1 as a representative of the series in mice, rats, and dogs was determined after i.v. and oral dosing. DprE1-IN-1 shows oral bioavailabilities of 86% and 100% in rats and dogs, respectively. The oral exposures of DprE1-IN-1, assessed in infected animals, shows AUCs ranging from 166 to 240 uM . h, and free plasma concentrations were maintained above the MIC for 10 to 24 h. [2]

References:
[1]. Shirude PS, et al. Lead optimization of 1,4-azaindoles as antimycobacterial agents. J Med Chem. 2014 Jul 10;57(13):5728-37.
[2]. Chatterji M, et al. 1,4-azaindole, a potential drug candidate for treatment of tuberculosis. Antimicrob Agents Chemother. 2014 Sep;58(9):5325-31.