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.
For research use only. We do not sell to patients.
- CAS No.: 2320542-03-6
- Formula: C30H27F6N3O
- Molecular Weight:559.55
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- Protocols
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
Description
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 |
In Vitro
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
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.
Chemical Information
-
CAS No. 2320542-03-6
-
Molecular Weight 559.55
-
Formula 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
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Antimalarial agent-75 Related Classifications
HY-190446 Related Classifications
Powered by Bioz