| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
| 500mg | |||
| Other Sizes |
| Targets |
ELQ300 targets the Plasmodium falciparum mitochondrial cytochrome bc₁ complex (cyt bc1), specifically binding to and inhibiting the reducing (Qi) site of the complex. By inhibiting the bc₁ complex, ELQ300 disrupts the parasite's electron transport chain, leading to loss of mitochondrial membrane potential and ATP depletion. The compound is highly selective for the parasite enzyme over human mitochondrial complexes, with minimal cytotoxicity against human HepG2 cells.
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| ln Vitro |
ELQ-300 (0-70 nM, 21 d) has IC50 values of 6.6, 4.6, and 160 nM, respectively, which inhibit the growth of Plasmodium falciparum Dd2, Tm90-C2B, and D1 [1].
In vitro, ELQ300 is a potent inhibitor of the P. falciparum cytochrome bc₁ complex with an IC50 of 0.56 nM. It inhibits growth of P. falciparum strains Dd2, Tm90-C2B, and D1 with IC50s of 6.6, 4.6, and 160 nM, respectively. It is notably effective against clinical isolates of P. falciparum with an EC50 value of 1.0 nM. The compound shows potent antimalarial activity with high selectivity and minimal cytotoxicity against human cells. |
| ln Vivo |
In models of acute infection, ELQ-300 (1 and 10 mg/kg; administered orally once daily for 1 or 4 days) reduces Plasmodium yoelii growth [2]. In mice, ELQ-300 (10 and 20 mg/kg; orally administered once daily for 1 or 4 days) inhibits the spread of infection [2].
In vivo, ELQ300 is a potent and orally bioavailable antimalarial agent. It has demonstrated efficacy in mouse models of malaria, including Plasmodium yoelii infections. The compound's oral bioavailability and potent activity against drug-resistant strains make it a promising candidate for malaria treatment. Its activity against clinical isolates supports its potential for treating malaria in endemic regions. |
| Enzyme Assay |
In vitro enzyme assays for ELQ300 measure inhibition of cytochrome bc₁ complex activity. The bc₁ complex is isolated from P. falciparum mitochondria, and enzyme activity is measured spectrophotometrically by monitoring the reduction of cytochrome c at 550 nm in the presence of decylubiquinol. Various concentrations of ELQ300 are added to assess inhibition. IC50 values are calculated from dose-response curves. Selectivity for the parasite enzyme over human bc₁ is assessed using human mitochondrial preparations.
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| Cell Assay |
Cellular assays for ELQ300 use P. falciparum cultures in human red blood cells. Parasites are cultured with various concentrations of ELQ300 for 48-72 hours. Parasite growth is assessed by measuring [³H]hypoxanthine incorporation, SYBR Green I fluorescence, or microscopic examination of Giemsa-stained blood smears. IC50/EC50 values are calculated from dose-response curves. Cytotoxicity against human HepG2 cells is assessed using MTT or ATP-lite assays.
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| Animal Protocol |
Animal/Disease Models: P. yoelii-WT infected 6weeks old female CF-1 mice [2]
Doses: 1 and 10 mg/kg Route of Administration: po (oral gavage); 1 mg/kg one time/day for 4 days ; 10 mg/kg, one time/day for 1 day. Experimental Results: To inhibit Plasmodium yoelii, the ED50 values of 4-day dosing and 1-day dosing were 0.04 and 0.03 mg/kg respectively. Animal/Disease Models: P. yoelii-WT infected 6weeks old female CF-1 mice [2] Doses: 10 and 20 mg/kg Route of Administration: po (oral gavage); 10 mg/kg one time/day for 4 days ; 20 mg/kg, one time/day for 1 day. Experimental Results: Effective in preventing relapse in a 4-day dosing study in infected mice. In vivo animal studies for ELQ300 utilize mouse models of malaria, such as P. yoelii or P. berghei infections. The compound is administered orally at various doses. Parasitemia is monitored by microscopic examination of blood smears over time. Survival is recorded. Efficacy is compared to vehicle and reference antimalarials (e.g., chloroquine, artemisinin). Pharmacokinetic sampling is performed to correlate exposure with efficacy. |
| ADME/Pharmacokinetics |
ELQ300 is orally bioavailable. As a small molecule with molecular weight of 474.85 g/mol (C₂₄H₁₇ClF₃NO₄), it is well-absorbed after oral administration. The compound's pharmacokinetic properties support once-daily oral dosing for malaria treatment. It is metabolized in the liver and excreted. Detailed PK parameters (half-life, Cmax, AUC, bioavailability) have been characterized in preclinical studies. Its favorable PK supports its development as an antimalarial.
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| Toxicity/Toxicokinetics |
Preclinical toxicity of ELQ300 has been evaluated in standard toxicology studies to support antimalarial development. As a cytochrome bc₁ inhibitor, potential adverse effects may include mitochondrial toxicity, though selectivity for the parasite enzyme over human enzyme reduces this risk. The compound shows minimal cytotoxicity against human HepG2 cells. Standard toxicology studies would assess genotoxicity, repeat-dose toxicity, and safety pharmacology.
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| 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.
[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. |
| Additional Infomation |
ELQ300 is a potent, orally bioavailable antimalarial agent targeting the cytochrome bc₁ complex (Qi site). It has IC50 of 0.56 nM against the parasite bc₁ complex and inhibits P. falciparum strains with nM potency. It shows high selectivity and minimal human cytotoxicity. It is available for research purposes only.
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| Molecular Formula |
C24H17CLF3NO4
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| Molecular Weight |
475.844296216965
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| Exact Mass |
475.079
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| CAS # |
1354745-52-0
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| PubChem CID |
67016608
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| Appearance |
White to off-white solid powder
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| LogP |
6.9
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
33
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| Complexity |
730
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
WZDNKHCQIZRDKW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H17ClF3NO4/c1-13-22(23(30)18-11-19(25)21(31-2)12-20(18)29-13)14-3-5-15(6-4-14)32-16-7-9-17(10-8-16)33-24(26,27)28/h3-12H,1-2H3,(H,29,30)
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| Chemical Name |
6-chloro-7-methoxy-2-methyl-3-[4-[4-(trifluoromethoxy)phenoxy]phenyl]-1H-quinolin-4-one
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| Synonyms |
ELQ 300; ELQ-300; ELQ300
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~15.62 mg/mL (~32.83 mM)
H2O : < 0.1 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.25 mg/mL (4.73 mM) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 22.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1015 mL | 10.5077 mL | 21.0155 mL | |
| 5 mM | 0.4203 mL | 2.1015 mL | 4.2031 mL | |
| 10 mM | 0.2102 mL | 1.0508 mL | 2.1015 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
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