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GNF179
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。
GNF179图片
CAS NO:1261114-01-5
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

GNF179是8,8-dimethyl IP类似物,具有良好的体外代谢稳定性和体内口服生物相容性。

Cas No.1261114-01-5
Canonical SMILESCC1(C)C2=NC(C3=CC=C(F)C=C3)=C(NC4=CC=C(Cl)C=C4)N2CCN1C(CN)=O
分子式C22H23ClFN5O
分子量427.9
溶解度DMSO: ≥ 125 mg/mL (292.12 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

GNF179 is an optimized 8,8-dimethyl IP analog that exhibited the potency(4.8 nM against the multidrug resistant strain W2) in vitro metabolic stability and in vivo oral bioavailability.IC50 value: 4.8 nM [1]Target: Anti-parasitic agent GNF179 exhibits a low clearance (CL=22 ml/min/kg, ~25% of hepatic blood flow in mice), a large volume of distribution (steady-state volume of distribution, Vss=11.8 l/kg), a moderate residence time (MRT=9 hours) and suitable terminal half-life (t1/2=8.9 hours). GNF179 reduced Plasmodium berghei parasitemia levels by 99.7% with a single 100 mg/kg oral dose, and prolonged mouse survival by an average of 19 days. GNF179 was able to protect against an infectious P. berghei sporozoite challenge with a single oral dose at 15 mg/kg while NITD609 was not.

[1]. Meister S, et al. Imaging of Plasmodium liver stages to drive next-generation antimalarial drug discovery. Science. 2011 Dec 9;334(6061):1372-7.