SQ109
Based on 4 publication(s) in Google Scholar
SQ109 is a potent inhibitor of the trypomastigote form of the parasite, with IC50 for cell killing of 50±8 nM. SQ109, targets MmpL3, is an antitubercular agent.
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- Pureza: 99.58%
- No. CAS: 502487-67-4
- Fòrmula: C22H38N2
- Peso molecular:330.55
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Almacenamiento:Pure form -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Publications Citing Use of MedChemExpress (MCE) SQ109
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Actividad biológica
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Trypanosoma |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MCF7 | IC50 |
18 μM
Compound: 1, SQ109
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Cytotoxicity against human MCF7 cells assessed as growth inhibition by MTT assay
Cytotoxicity against human MCF7 cells assessed as growth inhibition by MTT assay
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[PMID: 24568559] |
SQ109 also inhibits extracellular epimastigotes (IC50, 4.6±1 μM) and the clinically relevant intracellular amastigotes (IC50, ~0.5 to 1 μM), with a selectivity index of ~10 to 20. SQ109 has little effect (EC50, ~80 μM) in a red blood cell hemolysis assay. Besides, SQ109 causes major ultrastructural changes in all three life cycle forms, as observed by light microscopy, scanning electron microscopy (SEM), and transmission electron microscopy (TEM)[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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 502487-67-4
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Appearance Solid-Liquid Mixture
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Peso molecular 330.55
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Fòrmula C22H38N2
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Color Light yellow to yellow
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SMILES
C/C(C)=C/CC/C(C)=C/CNCCNC1[C@H]2C[C@H]3C[C@@H]1C[C@H](C3)C2
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Synonyms
NSC 722041
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Pure form -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (4)
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Journal Impact Factor
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Most Recent
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ACS Infect Dis
Diphenylether-Modified 1,2-Diamines with Improved Drug Properties for Development against Mycobacterium tuberculosis. [Abstract]2016 Jul 8;2(7):500-8. PMID: 27626102 -
Antimicrob Agents Chemother
Protective mechanism of action of the antifungal drug naftifine against Mycobacterium abscessus infection. [Abstract]2026 Feb 4;70(2):e0110525. PMID: 41532771 -
Dis Model Mech
An anti-tuberculosis compound screen using a zebrafish infection model identifies an aspartyl-tRNA synthetase inhibitor. [Abstract]2021 Dec 1;14(12):dmm049145. PMID: 34643222 -
Solvente y solubilidad
DMSO : ≥ 25 mg/mL (75.63 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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: ≥ 2.5 mg/mL (7.56 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.56 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Protocolo
The LLC-MK2 cells are treated with SQ109 (2.5 to 20 μM) and incubated for 96 h at 37°C. Fresh RPMI 1640 medium containing only 10% FBS is added to the untreated samples as a control. To determine toxicity, the MTS/PMS assay is performed. The selectivity index of SQ109 is determined based on its activities against the trypomastigote and intracellular amastigote forms of T.cruzi, calculated as the ratio of the 50% cytotoxic concentration (CC50) of mammalian cells to the IC50 or 50% lysing concentration (LC50) of T.cruzi. All experiments are performed in duplicate. The means are determined from ≥3 experiments[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[2]
Female C57BL/6 mice (8 weeks old) are used. Oral treatment of mice with INH (25 mg/kg), ethambutol (EMB) (100 mg/kg) and SQ109 (0.1, 10 and 25 mg/kg) is initiated 20 days after inoculation. Control groups of infected but untreated mice are killed at the initiation of therapy (early controls) or at the end of the treatment period. There are six mice per group. Chemotherapy is given daily for 5 days per week until the mice are killed, 4 weeks after initiation of treatment. The spleen and lungs are aseptically removed and weighed. The organs are homogenized in 2 ml of sterile PBS containing 0.05% Tween-80. Homogenate samples from individual tissues are diluted 10-fold in PBS and plated on 7H10 agar dishes. Inoculated dishes are incubated at 37°C in ambient air for 3 weeks prior to calculation of CFU. Viable counts are converted to a logarithmic scale; readings are corrected to represent whole organ totals. The severity of infection and the effectiveness of the treatments are assessed by the survival rate, and the mean number of CFU in mouse organs.
Rats and Dogs[3]
Male Fischer rats (271-289 g) and beagle dogs (7.5-8.9 kg, two males and two females per dose group) are used. Rats are given either a single intravenous (i.v.) bolus dose of 1.5 mg/kg (9 mg/m2) or an oral dose of 13 mg/kg (78 mg/m2) of SQ109 (n=8 per dose group); rats are divided into subgroups consisting of four rats per subgroup. Rat blood (0.7 mL) is withdrawn from the jugular vein catheter at alternating time points from individual rats in each subgroup. Blood samples are collected at 2, 5, 10, 15 and 30 min and 1, 3, 6, 10 and 24 h after a single i.v. administration, or 5, 15 and 30 min and 1, 2, 4, 6, 10 and 24 h after a single oral administration. Each blood sample is centrifuged to separate plasma, which is then stored at −70°C until analysis. Beagle dogs are dosed by gavage at either 3.75 or 15 mg/kg (75 or 300 mg/m2), or intravenously at either 0.45 or 4.5 mg/kg (9 and 90 mg/m2). Dog blood (0.7 mL) is withdrawn from the jugular vein at 2, 5, 10, 20 and 30 min and 1, 2, 4, 8, 12, 18 and 24 h after a single i.v. administration, or 10, 20 and 30 min and 1, 2, 4, 8, 12, 18 and 24 h after a single oral administration.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (276 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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Instrucciones de manejo (2659 KB)
Referencias
[1]. Veiga-Santos P, et al. SQ109, a new drug lead for Chagas disease. Antimicrob Agents Chemother. 2015 Apr;59(4):1950-61. [Content Brief]
[2]. Jia L, et al. Pharmacodynamics and pharmacokinetics of SQ109, a new diamine-based antitubercular drug. Br J Pharmacol. 2005 Jan;144(1):80-7 [Content Brief]
[3]. Jia L, et al. Interspecies pharmacokinetics and in vitro metabolism of SQ109. Br J Pharmacol. 2006 Mar;147(5):476-85. [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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.0253 mL | 15.1263 mL | 30.2526 mL | 75.6315 mL |
| 5 mM | 0.6051 mL | 3.0253 mL | 6.0505 mL | 15.1263 mL | |
| 10 mM | 0.3025 mL | 1.5126 mL | 3.0253 mL | 7.5632 mL | |
| 15 mM | 0.2017 mL | 1.0084 mL | 2.0168 mL | 5.0421 mL | |
| 20 mM | 0.1513 mL | 0.7563 mL | 1.5126 mL | 3.7816 mL | |
| 25 mM | 0.1210 mL | 0.6051 mL | 1.2101 mL | 3.0253 mL | |
| 30 mM | 0.1008 mL | 0.5042 mL | 1.0084 mL | 2.5211 mL | |
| 40 mM | 0.0756 mL | 0.3782 mL | 0.7563 mL | 1.8908 mL | |
| 50 mM | 0.0605 mL | 0.3025 mL | 0.6051 mL | 1.5126 mL | |
| 60 mM | 0.0504 mL | 0.2521 mL | 0.5042 mL | 1.2605 mL |
SQ109 Related Classifications
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