| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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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].
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| 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].
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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. |
| 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. |
| 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 |
|---|---|
| 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.
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