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首页-小分子抑制剂&激动剂-Antibiotics and Antivirals-Parasite-DSM1465
DSM1465

Chemical Structure : DSM1465

CAS No.:

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DSM1465 (DSM-1465, DSM 1465)

货号: PC-23717Not For Human Use, Lab Use Only.

DSM1465 is a potent, selective inhibitor of P. falciparum dihydroorotate dehydrogenase (PfDHODH) with IC50 of 15 nM, inhibits P. falciparum 3D7 (Pf3D7) parasites in whole-cell assays with EC50 of 1.4 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

DSM1465 is a potent, selective inhibitor of P. falciparum dihydroorotate dehydrogenase (PfDHODH) with IC50 of 15 nM, inhibits P. falciparum 3D7 (Pf3D7) parasites in whole-cell assays with EC50 of 1.4 nM.
DSM1465 displays no inhibition of human DHODH (IC50>30 uM).
DSM1465 (1, 3, 10, and 30 mg/kg) showed impressive preliminary in vivo activity in the humanized SCID mouse P. falciparum efficacy model.

物理化学性质&存储条件

分子量 467.76
分子式 C17H12ClF6N5O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

(R)-3-(1-(5-Chloro-6-(trifluoromethyl)pyridin-3-yl)-2,2,2-trifluoro-1-hydroxyethyl)-6-cyclopropyl-2-methyl-2,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one

参考文献

1. Zhe Nie, et al. J Med Chem. 2024 Dec 22. doi: 10.1021/acs.jmedchem.4c02394.

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