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首页-小分子抑制剂&激动剂-Antibiotics and Antivirals-Parasite-MMV030084
MMV030084

Chemical Structure : MMV030084

CAS No.: 342434-07-5

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MMV030084 (MMV-030084)

货号: PC-72339Not For Human Use, Lab Use Only.

MMV030084 (MMV-030084) is a potent, specific P. falciparum cGMP-dependent protein kinase (PKG) inhibitor (Kdapp=9-16 nM), inhibits invasion of P. berghei ANKA parasites into HepG2 liver cells with IC50 of 199 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    MMV030084 (MMV-030084) is a potent, specific P. falciparum cGMP-dependent protein kinase (PKG) inhibitor (Kdapp=9-16 nM), inhibits invasion of P. berghei ANKA parasites into HepG2 liver cells with IC50 of 199 nM.
    MMV030084 potently inhibits hepatocyte invasion by Plasmodium sporozoites, merozoite egress from asexual blood stage schizonts, and male gamete exflagellation, shows potent activity against liver, asexual, and sexual blood stage development.
    MMV030084 showed an IC50 of 109 nM against the drug-sensitive 3D7-A10 line, and an IC50 of 120 nM against multidrug-resistant Dd2-B2 parasites in a 72-h growth inhibition assay against Pf ABS parasites.
    MMV030084 inhibited male gamete exflagellation at an IC50 of 141 nM when gametocytes were stimulated to develop into male gametes.
    MMV030084 is a promising Plasmodium PKG-targeting chemotype.

    物理化学性质&存储条件

    分子量 342.827
    分子式 C18H19ClN4O
    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

    5-(2-(1-amino-2-methylpropan-2-yl)-5-(pyridin-4-yl)-1H-imidazol-4-yl)-2-chlorophenol

    参考文献

    1. Manu Vanaerschot, et al. Cell Chem Biol. 2020 Jul 16;27(7):806-816.e8.

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