HLQ-102
HLQ-102 is an orally active parasite cytochrome bc1 complex Qi site binder. HLQ-102 inhibits the growth of Plasmodium. HLQ-102 exhibits antimalarial activity against Plasmodium in mice. HLQ-102 can be used in malaria-related research.
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- Formule: C24H17ClF3NO4
- Masse moléculaire:475.84
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Stockage:
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]
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
HLQ-102 (Compound 1a) potently inhibits the growth of *Plasmodium falciparum* strains D6, Dd2 and Tm90-C2B with sub-nanomolar IC50 values, but shows no activity against the ELQ-300-resistant D1 strain, indicating that it targets the Qi site of the parasite cytochrome bc1 complex[1].
HLQ-102 (48 h) inhibits liver-stage replication of *Plasmodium berghei* in HepG2 cells, with an IC50 of 3.6 nM[1].
In prophylactic mode, HLQ-102 inhibits schizont formation of *Plasmodium cynomolgi* in non-human primate hepatocytes with an IC50 of 47 nM, but it does not target hypnozoites or established liver-stage parasites, and shows no cytotoxicity at concentrations up to 1000 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | Cmax | Tmax | T1/2 | AUC0-inf | MRT0-inf | F | Vdss | CL |
|---|---|---|---|---|---|---|---|---|---|---|
| Mice[1] | 0.41 mg/kg | i.v. | 345 ng/mL | 0.25 h | 3.16 h | 1485 ng·h/mL | 4.87 h | 100 % | / | / |
| Mice[1] | 8.23 mg/kg | p.o. | 1513 ng/mL | 8.00 h | 4.95 h | 25116 ng·h/mL | 10.2 h | 85 % | / | / |
| Rat[1] | 0.5 mg/kg | i.v. | / | / | 6.22 h | 6360 ng·h/mL | 7.67 h | 100 % | 0.602 L/kg | 0.0789 L/h/kg |
| Rat[1] | 8.23 mg/kg | p.o. | 2393 ng/mL | 8.00 h | 7.34 h | 42314 ng·h/mL | 11.9 h | 40 % | / | / |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CF1 mice (female, 28-30 g, 8-10 weeks old, inoculated intravenously with 3.5 × 104 Plasmodium yoelii-parasitized erythrocytes)[1]
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Dosage:0.0025, 0.005, 0.01, 0.03, 0.1, 0.3,
1.0, and 10 mg/kg/day -
Administration:p.o.; daily; 4 days
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Result:Achieved an ED50 of 0.01 mg/kg/day.
Achieved an ED90 of 0.075 mg/kg/day.
Achieved a Non-Recrudescence Dose (NRD) of 3 mg/kg/day.
Chemical Information
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Masse moléculaire 475.84
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Formule C24H17ClF3NO4
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SMILES
O=C1C(C)=C(C2=CC=C(OC3=CC=C(OC(F)(F)F)C=C3)C=C2)NC4=CC(OC)=C(Cl)C=C41
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
HLQ-102 Related Classifications
HY-184395 Related Classifications
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- HLQ-102
- HLQ102
- HLQ 102
- Parasite
- human fibroblasts
- Plasmodium cynomolgi schizonts
- drug-resistant Plasmodium falciparum blood-stage parasites
- cytochrome bc1 complex Qi site
- Plasmodium yoelii
- Plasmodium falciparum
- murine malaria
- Plasmodium berghei hepatic schizonts
- bovine cytochrome bc1 complex
- Hep-G2 cells
- Inhibitor
- inhibitor
- inhibit