ISPA-28

Names

[ Name ]:
ISPA-28

[Synonym ]:
5-Isoxazolecarboxamide, N-(2,3-dihydro-1,5-dimethyl-3-oxo-2-phenyl-1H-pyrazol-4-yl)-3-(1-ethyl-3-methyl-1H-pyrazol-4-yl)-4,5-dihydro-
N-(1,5-Dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazol-4-yl)-3-(1-ethyl-3-methyl-1H-pyrazol-4-yl)-4,5-dihydro-1,2-oxazole-5-carboxamide
MFCD08106635

Biological Activity

[Description]:

ISPA-28 is a specific plasmodial surface anion channel (PSAC) antagonist. ISPA-28 binds directly and reversibly to CLAG3[1][2].

[Related Catalog]:

Research Areas >> Infection

[In Vitro]

ISPA-28 is only effective as an inhibitor of Dd2 channels (K0.5 values of 56 nM and 43 μM for Dd2 and HB3 channels, respectively)[2].

[References]

[1]. Sanjay A Desai, et al. Ion and Nutrient Uptake by Malaria Parasite-Infected Erythrocytes.

[2]. Wang Nguitragool, et al. Proteolysis at a Specific Extracellular Residue Implicates Integral Membrane CLAG3 in Malaria Parasite Nutrient Channels.

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Molecular Formula ]:
C₂₁H₂₄N₆O₃

[ Molecular Weight ]:
408.454

[ Exact Mass ]:
408.190979

[ LogP ]:
0.18

[ Index of Refraction ]:
1.672

Safety Information

[ RIDADR ]:
NONH for all modes of transport

Articles

An epigenetic antimalarial resistance mechanism involving parasite genes linked to nutrient uptake.

J. Biol. Chem. 288(27) , 19429-40, (2013)

Acquired antimalarial drug resistance produces treatment failures and has led to periods of global disease resurgence. In Plasmodium falciparum, resistance is known to arise through genome-level chang...

Malaria parasite mutants with altered erythrocyte permeability: a new drug resistance mechanism and important molecular tool.

Future Microbiol. 5(1) , 81-97, (2010)

Erythrocytes infected with plasmodia, including those that cause human malaria, have increased permeability to a diverse collection of organic and inorganic solutes. While these increases have been kn...

Related Compounds

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