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首页-小分子抑制剂&激动剂-Antibiotics and Antivirals-Parasite-EDI048
EDI048

Chemical Structure : EDI048

CAS No.: 2767264-57-1

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EDI048 (NVP-EDI048, EDI-048)

货号: PC-23131Not For Human Use, Lab Use Only.

EDI048 (EDI-048) is a specific, ATP-competitive, gastrointestinal-targeted Cryptosporidium PI(4)K (CpPI(4)K) inhibitor with IC50 of 4 nM, >300-fold with human orthologue HsPI(4)K, demonstrates in vitro anti-Cryptosporidium activity (Cp CPE, EC50=52 nM).

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10 mg ￥3580 In stock
25 mg ￥5980 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

EDI048 (EDI-048) is a specific, ATP-competitive, gastrointestinal-targeted Cryptosporidium PI(4)K (CpPI(4)K) inhibitor with IC50 of 4 nM, >300-fold with human orthologue HsPI(4)K, demonstrates in vitro anti-Cryptosporidium activity (Cp CPE, EC50=52 nM).
EDI048 is a potent CpPI(4)K inhibitor (IC50 = 5.2 nM) with anti-parasitic activity against both C. parvum and C. hominis, is active on Cryptosporidium in the gastrointestinal epithelium in the mouse model.
EDI048 demonstrated dose-dependent efficacy with a 0.3, 1.1 and 3.1 log reduction in oocyst shedding at 1, 3 and 10 mg kg−1 doses, respectively.
EDI048 is a soft drug in all tested preclinical species and had no human-specific metabolites, warranting further safety and efficacy profiling.
EDI048 blocks membrane biogenesis, preventing the formation of functional merozoites.

物理化学性质&存储条件

分子量 476.92
分子式 C25H21ClN4O4
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

methyl 2-chloro-5-(N-methyl-3-(4-(methylcarbamoyl)phenyl)pyrazolo[1,5-a]pyridine-5-carboxamido)benzoate

参考文献

1. Manjunatha UH, et al. Nat Microbiol. 2024 Oct 8. doi: 10.1038/s41564-024-01810-x.

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