ELQ-300
Based on 1 Customer Validation
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.
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- Purity: 98.0%
- CAS No.: 1354745-52-0
- 화학식: C24H17ClF3NO4
- 분자량:475.84
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
All Parasite Isoforms
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Biological Activity
IC50: 6.6 nM (P. falciparum Dd2), 4.6 nM (P. falciparum Tm90-C2B), 160 nM (P. falciparum D1)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
>10 μM
Compound: 7, ELQ-300
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Inhibition of human cytochrome bc1 complex derived from HEK293 cell mitochondria using 50 uM decylubiquinol as substrate
Inhibition of human cytochrome bc1 complex derived from HEK293 cell mitochondria using 50 uM decylubiquinol as substrate
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[PMID: 24720377] |
| HepG2 | IC50 |
>10 μM
Compound: 7, ELQ-300
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Cytotoxicity against human HepG2 cells after 24 hrs incubation by Alamar Blue assay
Cytotoxicity against human HepG2 cells after 24 hrs incubation by Alamar Blue assay
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[PMID: 24720377] |
| HepG2 | IC50 |
>10 μM
Compound: ELQ-300
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Cytotoxicity against human HepG2 cells
Cytotoxicity against human HepG2 cells
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[PMID: 33131885] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:6-week female CF-1 mice with P. yoelii-WT infection[2]
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Dosage:1 and 10 mg/kg
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Administration:Oral gavage; 1 mg/kg once daily for 4-day; 10 mg/kg once daily for 1-day
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Result:Inhibited P. yoelii with ED50 values of 0.04 and 0.03 mg/kg for 4-day dosing and 1-day dosing, respectively.
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Animal Model:6-week female CF-1 mice with P. yoelii-WT infection[2]
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Dosage:10 and 20 mg/kg
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Administration:Oral gavage; 10 mg/kg once daily for 4-day; 20 mg/kg once daily for 1-day
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Result:Effectively prevented recrudescence in the 4-day dosing studies with infection mice.
Chemical Information
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CAS No. 1354745-52-0
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Appearance Solid
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분자량 475.84
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화학식 C24H17ClF3NO4
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Color White to off-white
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SMILES
O=C1C(C2=CC=C(OC3=CC=C(OC(F)(F)F)C=C3)C=C2)=C(C)NC4=C1C=C(Cl)C(OC)=C4
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
용액&용해도
DMSO : 15.62 mg/mL (32.83 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.25 mg/mL (4.73 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.25 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (22.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (272 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1015 mL | 10.5077 mL | 21.0155 mL | 52.5387 mL |
| 5 mM | 0.4203 mL | 2.1015 mL | 4.2031 mL | 10.5077 mL | |
| 10 mM | 0.2102 mL | 1.0508 mL | 2.1015 mL | 5.2539 mL | |
| 15 mM | 0.1401 mL | 0.7005 mL | 1.4010 mL | 3.5026 mL | |
| 20 mM | 0.1051 mL | 0.5254 mL | 1.0508 mL | 2.6269 mL | |
| 25 mM | 0.0841 mL | 0.4203 mL | 0.8406 mL | 2.1015 mL | |
| 30 mM | 0.0701 mL | 0.3503 mL | 0.7005 mL | 1.7513 mL |
ELQ-300 Related Classifications
HY-13836 Related Classifications
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