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首页-小分子抑制剂&激动剂-Antibiotics and Antivirals-Bacterial-MK-7602
MK-7602

Chemical Structure : MK-7602

CAS No.: 2606991-88-0

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MK-7602 (MK7602)

货号: PC-25967Not For Human Use, Lab Use Only.

MK-7602 is a potent multi-stage dual-targeting antimalarial compound, is a dual inhibitor of plasmepsins IX and X with Ki of 0.132 nM and 0.683 nM for PfPMX and PfPMIX respectively, inhibits inhibit asexual growth of P. falciparum with EC50 of 0.4 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

MK-7602 is a potent multi-stage dual-targeting antimalarial compound, is a dual inhibitor of plasmepsins IX and X with Ki of 0.132 nM and 0.683 nM for PfPMX and PfPMIX respectively, inhibits inhibit asexual growth of P. falciparum with EC50 of 0.4 nM.
MK-7602 is a potent dual inhibitor of the aspartic protease activity of both P. falciparum PMIX (PfPMIX) (Ki 0.68 nM) and PMX (PfPMX) (Ki 0.13 nM) and it also inhibited PMX from both P. vivax (PvPMX) (Ki 0.03 nM) and P. knowlesi (PkPMX) (Ki 0.09 nM).
MK-7602 has strong selectivity for dual inhibition of PfPMIX and PfPMX compared to other aspartic proteases including P. vivax plasmepsin V (PvPMV) (174,374-fold, PMV/PMX) and the human proteases BACE1 (>43,426-fold, BACE1/PMX), cathepsin D (CatD) (21,443-fold, CatD/PMX) and renin (4250-fold, renin/PMX).
MK-7602 displays >4000-fold selectivity versus these human proteases.
MK-7602 inhibits P. falciparum development in the blood stage, inhibits P. falciparum blood stage parasite growth.
MK-7602 is effective against blood stage P. berghei mouse models of malaria.

物理化学性质&存储条件

分子量 518.66
分子式 C30H38N4O4
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

(2S,3S)-3-(2-amino-4,4-diethyl-6-oxo-5,6-dihydropyrimidin-1(4H)-yl)-N-((1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl)-2-(methoxymethyl)-2-methyl-2,3-dihydro-1H-indene-5-carboxamide

参考文献

1. Favuzza P, et al. EBioMedicine. 2026 Jan;123:106061.

2. Stanley SE, et al. Antimicrob Agents Chemother. 2026 Jan 14:e0126125.

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