| Identification | Back Directory | [Name]
ELQ－300 | [CAS]
1354745-52-0 | [Synonyms]
ELQ－300
ELQ300; ELQ-300; ELQ 300
6-chloro-7-methoxy-2-methyl-3-[4-[4-(trifluoromethoxy)phenoxy]phenyl]-1H-quinolin-4-one
4(1H)-Quinolinone, 6-chloro-7-methoxy-2-methyl-3-[4-[4-(trifluoromethoxy)phenoxy]phenyl]- | [Molecular Formula]
C24H17ClF3NO4 | [MDL Number]
MFCD28386233 | [MOL File]
1354745-52-0.mol | [Molecular Weight]
475.84 |
| Chemical Properties | Back Directory | [Boiling point ]
551.2±50.0 °C(Predicted) | [density ]
1.362±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: 15.62 mg/mL (32.83 mM); Water: < 0.1 mg/mL (insoluble) | [form ]
Solid | [pka]
0.88±0.70(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
ELQ-300 is a potent and orally bioavailable antimalarial agent, acts as an inhibitor of the reductive (Qi) site of the cytochrome bc1 complex (cyt bc1). ELQ-300 inhibits growth of P. falciparum Dd2, Tm90-C2B, and D1 with IC50 values of 6.6, 4.6 and 160 nM, respectively. ELQ-300 can be used for the research of antimalarial[1][2]. | [in vivo]
ELQ-300 (1 and 10 mg/kg; p.o. once daily for 1 or 4 days) inhibits P. yoelii growth in an acute infection model[2].
ELQ-300 (10 and 20 mg/kg; p.o. once daily for 1 or 4 days) prevents recurrence of infection in mice[2]. | Animal Model: | 6-week female CF-1 mice with P. yoelii-WT infection[2] | | Dosage: | 1 and 10 mg/kg | | Administration: | Oral gavage; 1 mg/kg once daily for 4-day; 10 mg/kg once daily for 1-day | | Result: | Inhibited P. yoelii with ED50 values of 0.04 and 0.03 mg/kg for 4-day dosing and 1-day dosing, respectively. |
| Animal Model: | 6-week female CF-1 mice with P. yoelii-WT infection[2] | | Dosage: | 10 and 20 mg/kg | | Administration: | Oral gavage; 10 mg/kg once daily for 4-day; 20 mg/kg once daily for 1-day | | Result: | Effectively prevented recrudescence in the 4-day dosing studies with infection mice. |
| [References]
[1] Stickles AM, et al. Subtle changes in endochin-like quinolone structure alter the site of inhibition within the cytochrome bc1 complex of Plasmodium falciparum. Antimicrob Agents Chemother. 2015 Apr;59(4):1977-82. DOI:10.1128/AAC.04149-14
[2] Stickles AM, et al. Atovaquone and ELQ-300 Combination Therapy as a Novel Dual-Site Cytochrome bc1 Inhibition Strategy for Malaria. Antimicrob Agents Chemother. 2016 Jul 22;60(8):4853-9. DOI:10.1128/AAC.00791-16 |
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| Company Name: |
SPIRO PHARMA
|
| Tel: |
|
| Website: |
www.spiropharma.com.cn |
| Company Name: |
BOC Sciences
|
| Tel: |
16314854226 |
| Website: |
www.bocsci.com |
|