LSPN959
LSPN959 is a slow-acting indole peptidomimetic antiplasmodial agent with submicromolar activity against the Plasmodium falciparum 3D7 strain. LSPN959 does not inhibit plastid-dependent isoprenoid biosynthesis. The combination of LSPN959 with Artesunate (HY-N0193) exhibits an additive effect against Plasmodium falciparum. LSPN959 can be used in malaria research.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 分子式: C34H37BrN4O3
- 分子量:629.59
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
製品説明
体外実験
LSPN959 (0.049-50 μM; 72 h) potently inhibits chloroquine-sensitive Plasmodium falciparum 3D7 strain growth with an IC50 of 1.05 μM, exhibits low cytotoxicity against human HepG2 and HEK293 cells, and has a high selectivity index of 95[1].
LSPN959 (0.049-50 μM; 24-72 h) exhibits a slow-acting inhibitory profile against Plasmodium falciparum 3D7 strain, with IC50 ratios and morphological observations consistent with delayed parasite killing and recovery potential post-exposure[1].
LSPN959 (72 h)'s antiplasmodial activity against Plasmodium falciparum 3D7 strain is not reversed by IPP supplementation, indicating it does not inhibit apicoplast-dependent isoprenoid biosynthesis[1].
LSPN959 (72 h) exhibits an additive interaction when combined with Artesunate against Plasmodium falciparum 3D7 strain, with no statistically significant synergy or antagonism observed[1].
LSPN959 (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, showing no cross-resistance with standard antimalarials[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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分子量 629.59
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分子式 C34H37BrN4O3
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SMILES
CC(C)(NC(CN(C(C1=CC=CC=C1)=O)CC(C2=CC3=CC=CC=C3N2C(N4CCCC4)=O)C5=CC=C(C=C5)Br)=O)C
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Keywords
- LSPN959
- LSPN 959
- LSPN-959
- Parasite
- Plasmodium falciparum 3D7
- malaria
- human HEK293 cells
- human cells
- artesunate
- human HepG2 cells
- apicoplast-dependent isoprenoid biosynthesis
- drug-resistant Plasmodium falciparum strains
- chloroquine-sensitive Plasmodium falciparum 3D7 strain
- isopentenyl pyrophosphate
- Inhibitor
- inhibitor
- inhibit