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DSM502
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。
DSM502图片
CAS NO:2426616-55-7
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议

产品介绍
DSM502 是一种基于吡咯的二氢乳清酸脱氢酶 (DHODH) 抑制剂。DSM502 对 Plasmodium DHODH 和 Plasmodium 寄生虫表现出纳摩尔级效力,对哺乳动物 DHODH 没有抑制作用。
Cas No.2426616-55-7
分子式C16H16F3N3O
分子量323.31
溶解度DMSO : 250 mg/mL (773.25 mM; Need ultrasonic)
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

DSM502 is a pyrrole-based Dihydroorotate Dehydrogenase (DHODH) inhibitor. DSM502 exhibits nanomolar potency againsts Plasmodium DHODH and Plasmodium parasites, with no inhibition of mammalian DHODHs[1].

DSM502 shows inhibitory activity against P. falciparum DHODH (PfDHODH, IC50=20 nM), P. vivax DHODH (PvDHODH, IC50=14 nM) and Pf3D7 cells (EC50=14 nM), with no inhibition of the human enzyme[1].

DSM502 (10 and 50 mg/kg; p.o. once daily for 4 days) results in 97% parasite clearance in confirmatory SCID study compared to 85% clearance in the GSK study[1].DSM502 (18.3 and 50 mg/kg; a single p.o.) exhibits high oral bioavailability (>100%, >100%), apparent t1/2 (2.6, 3.6 h) and Cmax (8.4, 42.3 μM) in mice[1].DSM502 (2.8 mg/kg; a single i.v.) exhibits apparent t1/2 (2.8 h), plasma clearance (26.1 mL/min/kg), and Vss (1.2 L/kg) in mice[1].

[1]. Kokkonda S, et, al. Lead Optimization of a Pyrrole-Based Dihydroorotate Dehydrogenase Inhibitor Series for the Treatment of Malaria. J Med Chem. 2020 May 14;63(9):4929-4956.
[2]. Palmer MJ, et, al. Potent Antimalarials with Development Potential Identified by Structure-Guided Computational Optimization of a Pyrrole-Based Dihydroorotate Dehydrogenase Inhibitor Series. J Med Chem. 2021 May 13;64(9):6085-6136.