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| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
DSM502, 恶性疟原虫二氢烟酸脱氢酶
有货
为什么选择此级别
Moligand™ 级 ，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
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
In Vitro
DSM502 shows inhibitory activity against P. falciparum DHODH ( Pf DHODH, IC 50 =20 nM), P. vivax DHODH ( Pv DHODH, IC 50 =14 nM) and Pf 3D7 cells (EC 50 =14 nM), with no inhibition of the human enzyme. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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 t 1/2 (2.6, 3.6 h) and C max (8.4, 42.3 μM) in mice . DSM502 (2.8 mg/kg; a single i.v.) exhibits apparent t 1/2 (2.8 h), plasma clearance (26.1 mL/min/kg), and V ss (1.2 L/kg) in mice . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: SCID mice (23-36 g) were inoculated with parasites Dosage: 10 and 50 mg/kg Administration: P.o. once daily for 4 days starting on day 3 after mice had been inoculated with parasites Result: Resulted in 97% parasite clearance compared to 85% clearance in the GSK study. The 10 mg/kg mouse died on day 5.
IC50& Target:Plasmodium
规格
规格或纯度
Moligand™, 10mM in DMSO
英文名称
DSM502
生化机理
DSM502 是一种基于吡咯的二氢烟酸脱氢酶 (DHODH) 抑制剂。DSM502 对疟原虫 DHODH 和疟原虫具有纳摩尔效力，对哺乳动物的 DHODH 没有抑制作用。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
作用机制
恶性疟原虫二氢烟酸脱氢酶
名称和识别符
分子类型
小分子
分子量
323.31
技术文档
高级数据
关联靶点（人）
DHODH
Tclin
二氢乳清酸脱氢酶（醌），线粒体(Dihydroorotate dehydrogenase (quinone), mitochondrial)
(0 活性数据)
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
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技术文档和文章
溶液计算器
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