耗材描述
DSM502
产品活性: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。
产品来源: https://www.medchemexpress.cn/dsm502.html
研究领域:Metabolic Enzyme/Protease | Anti-infection
作用靶点:Dihydroorotate Dehydrogenase | Parasite
In Vitro: 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.
In Vivo: 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.
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.
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.
相关产品:Bioactive Compound Library Plus | Anti-Infection Compound Library | Metabolism/Protease Compound Library | Ferroptosis Compound Library | Orally Active Compound Library | Antiparasitic Compound library | Mitochondria-Targeted Compound Library | Heterocyclic Compound Library | Metabolic Enzyme Compound Library | Multi-Target Compound Library | Bioactive Compound Library Max | Chloroquine | Puromycin dihydrochloride | Hygromycin B | Doxycycline hyclate | Acetaminophen | Anisomycin | Metronidazole | Kaempferol | Amphotericin B | Hydroxychloroquine | Brequinar | Monensin sodium | Dihydroartemisinin | Niclosamide | Berberine chloride | Artesunate | Acridine Orange hydrochloride | Ivermectin | Eflornithine hydrochloride hydrate | Azithromycin | TPE-MI | Halofuginone | Ibuprofen | Artemisinin | 5'-Methylthioadenosine | Leflunomide | RRx-001
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