Antimalarial agent-75
Antimalarial agent-75 is an antimalarial agent. Antimalarial agent-75 antagonizes DRD2S, blocks GluN1A/GluN2B NMDA receptor channels, weakly blocks GABA-A channels, and moderately inhibits AChE. Antimalarial agent-75 inhibits Chloroquine (HY-17589A)-sensitive and -resistant Plasmodium falciparum strains, and reduces parasitemia in the Plasmodium berghei ANKA-infected mouse model. Antimalarial agent-75 can be used for research on malaria.
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。
- CAS 番号: 2320542-03-6
- 分子式: C30H27F6N3O
- 分子量:559.55
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
IC50 & Target
[1]|
Plasmodium |
AChE |
NMDA Receptor |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HepG2 | CC50 |
2.7 μM
|
Cytotoxicity against human hepatocarcinoma HepG2 cells assessed by CellTiter-Glo luminescent cell viability assay after 48 hrs incubation.
Cytotoxicity against human hepatocarcinoma HepG2 cells assessed by CellTiter-Glo luminescent cell viability assay after 48 hrs incubation.
|
42800114 |
| HFF | CC50 |
5.0 μM
|
Cytotoxicity against human foreskin fibroblast HFF cells assessed by CellTiter-Glo luminescent cell viability assay after 48 hrs incubation.
Cytotoxicity against human foreskin fibroblast HFF cells assessed by CellTiter-Glo luminescent cell viability assay after 48 hrs incubation.
|
42800114 |
体外実験
Antimalarial agent-75 has a low intrinsic clearance (5.1 µL/min/mg) in human liver microsomes, with the longest half-life of 279.7 min; it also shows weak inhibition of major CYP subtypes, with inhibition rates not exceeding 16.3%[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c ByJ (female, 7-8 weeks old, average body weight approximately 24 g, injected with 200 μL of a 0.9% NaCl solution containing 106-107 P. berghei parasitized murine erythrocytes)
[1] -
Dosage:5 mg/kg/day
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Administration:i.p.; once daily; for 5 consecutive days
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Result:Reduced parasitemia by at least 60% relative to the negative control group by Day 5 of dosing, maintaining parasitemia below 0.36% after five days of treatment, and yielded a 71% survival rate for treated mice at Day 30.
化学情報
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CAS 番号 2320542-03-6
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分子量 559.55
-
分子式 C30H27F6N3O
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SMILES
O[C@@H](C1=CC(C(F)(F)F)=NC(C2=CC=C(C(F)(F)F)C=C2)=C1)CNCCNC(C3=CC=CC=C3)C4=CC=CC=C4
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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)