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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
화학식: C₃₀H₂₇F₆N₃O
분자량:559.55

보관:

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

Antimalarial agent-75 Chemical Structure

CAS No.: 2320542-03-6

Amount: USD 0.00

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Use of MCE Products

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

Biological Activity
- 제품 설명
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

IC₅₀ & Target

^[1]

Plasmodium

AChE

NMDA Receptor

All Parasite Isoforms :

All Cholinesterase (ChE) Isoforms :

AChE
BChE

All iGluR Isoforms :

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
분자량 559.55
화학식 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
선적

Room temperature in continental US; may vary elsewhere.
보관

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

순도&문서

Handling Instructions (2659 KB)

References

[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

몰농도 계산기

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

MOQ

Minimum order quantity

100 mg

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Amount: USD 0.00

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
순도&문서
References

상품명:
Cat. No.:
수량:
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Antimalarial agent-75

All Parasite Isoforms

All Cholinesterase (ChE) Isoforms

All iGluR Isoforms