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Cat. No.: HY-190446

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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.

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CAS No.: 2320542-03-6
Formule: C₃₀H₂₇F₆N₃O
Masse moléculaire:559.55

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Please store the product under the recommended conditions in the Certificate of Analysis.

Antimalarial agent-75 Chemical Structure

CAS No.: 2320542-03-6

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
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Activité biologique

Description

IC₅₀ & Target

^[1]

Plasmodium

AChE

NMDA Receptor

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AChE
BChE

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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

In Vitro

Anti-cancerGlutamate Release or ReceptorsParasitic InfectionOthers

Anti-cancer

Antimalarial agent-75 (0-100 µM; 48 h) is cytotoxic to HepG2 and HFF cells, with CC₅₀ values of 2.7 µM and 5.0 µM, respectively, corresponding to selectivity indices higher than 300^[1].

Glutamate Release or Receptors

Antimalarial agent-75 shows the strongest interactions with NET (78.55%), DAT (78.85%), and DRD2S antagonism (77.5%) in cell-based CNS interaction assays, with lower activity against most other tested targets; it also produces mild 15.2% inhibition of AChE^[1].

Parasitic Infection

Antimalarial agent-75 (compound 10a) inhibits P. falciparum Pf3D7 and PfW2, with IC₅₀ values of 8.7 nM and 3.7 nM, respectively^[1].

Others

Antimalarial agent-75 (0.1-10 µM) shows minimal inhibition of hERG at 0.1 and 1 µM, but produces 79.8% inhibition of hERG in CHO-K1 cells at 10 µM^[1].
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.

In Vivo

Parasitic Infection

Antimalarial agent-75 (compound 10a) (5 mg/kg/day; i.p.; once daily; for 5 consecutive days) reduces parasitemia and achieves a 71% Day 30 survival rate in P. berghei ANKA-infected mice^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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
Administration:

i.p.; once daily; for 5 consecutive days
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.

Related Protocols :

How to Choose the Right Model Animal

Chemical Information

CAS No. 2320542-03-6
Masse moléculaire 559.55
Formule C₃₀H₂₇F₆N₃O
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
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

Please store the product under the recommended conditions in the Certificate of Analysis.

Pureté et documentation

Instruction de manipulation (2659 KB)

Références

[1]. Herrero A, et al. Novel enantiopure pyridine-based aminoalcohols as promising antimalarial candidates. European journal of medicinal chemistry. 2026 Sep 24;320:119349.

Calculators

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Activité biologique
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- In Vivo
Chemical Information
Pureté et documentation
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Antimalarial agent-75

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