LSPN954
LSPN954 is an indole-based peptidomimetic antiplasmodial agent. LSPN954 shows slow-acting inhibitory activity, allowing the initial development of Plasmodium followed by morphological changes. LSPN954 can be used in malaria research.
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- Formel: C35H40N4O3
- Molecular Weight:564.72
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
LSPN954 (compound 4i) (0.049-50 μM; 72 h for P. falciparum; 1.56-100 μM; 72 h for HepG2) potently inhibits Plasmodium falciparum 3D7 growth with an IC50 of 1.7 μM, shows low cytotoxicity against human HepG2 and HEK293 cells, and has high selectivity indices of 59 and >59, respectively[1].
LSPN954 (0.049-50 μM; 24, 48, 72 h exposure periods; 10× IC50; 24 h morphological analysis) exhibits slow-acting inhibitory activity against Plasmodium falciparum 3D7, as shown by IC50 ratios above 1 for 24 h vs 72 h exposure and a 4-fold ratio for 6-day vs 4-day regrowth, plus morphological evidence of parasite recovery after initial exposure[1].
LSPN954 (0.01-100 μM; 72 h, with 200 μM IPP co-treatment) antiplasmodial activity against Plasmodium falciparum 3D7 is not reversed by IPP supplementation, indicating its activity does not involve inhibition of apicoplast-dependent isoprenoid biosynthesis[1].
LSPN954 (0.049-50 μM; 72 h) retains potent antiplasmodial activity against multidrug-resistant Plasmodium falciparum strains (3D7R_MMV848, Dd2R_DSM265, Dd2, K1, TM90C6B) with resistance indices close to 1, indicating no cross-resistance with standard antimalarials[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Molecular Weight 564.72
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Formel C35H40N4O3
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SMILES
CC1=CC=C(C=C1)C(C2=CC3=CC=CC=C3N2C(N4CCCC4)=O)CN(C(C5=CC=CC=C5)=O)CC(NC(C)(C)C)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)