| Bioactivity | 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]. | ||||||||||||
| Target | IC50: 6.6 nM (P. falciparum Dd2), 4.6 nM (P. falciparum Tm90-C2B), 160 nM (P. falciparum D1) | ||||||||||||
| Invitro | ELQ-300 (0-70 nM, 21 d) inhibits P. falciparum Dd2, Tm90-C2B, and D1 growth with IC50 values of 6.6, 4.6 and 160 nM, respectively[1]. | ||||||||||||
| 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: | ||||||||||||
| Name | ELQ-300 | ||||||||||||
| CAS | 1354745-52-0 | ||||||||||||
| Formula | C24H17ClF3NO4 | ||||||||||||
| Molar Mass | 475.84 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. [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. |
ELQ-300
CAS: 1354745-52-0 F: C24H17ClF3NO4 W: 475.84
ELQ-300 is a potent and orally bioavailable antimalarial agent, acts as an inhibitor of the reductive (Qi) site of the c
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