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Synonyms: NSC 722041


| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 1 mg | $50 | - | In Stock | |
| 5 mg | $118 | In Stock | In Stock | |
| 10 mg | $182 | In Stock | In Stock | |
| 25 mg | $367 | In Stock | In Stock | |
| 50 mg | $548 | In Stock | In Stock | |
| 100 mg | $828 | In Stock | In Stock | |
| 1 mL x 10 mM (in DMSO) | $128 | - | In Stock |
| Description | SQ109 (NSC 722041) is an ethambutol (EMB) derivative and a specific inhibitor of MmpL3, exhibiting potent anti-Mycobacterium tuberculosis activity. SQ109 effectively inhibits the adult stage of the parasite Trypanosoma and kills cells, with an IC50 of 50 ± 8 nM. SQ109 can be used in tuberculosis and antiparasitic research. |
| Targets & IC50 | CYP142:52 ± 11 µM (Kd), ferredoxin (Trichomonas vaginalis):3.15 µM, CYP125:41 ± 3 µM (Kd), Parasite:50 nM (trypomastigote cell), CYP124:3.4 ± 0.3 µM (Kd) |
| In vitro | Methods: Peritoneal macrophages from mice were infected with M.tb H37Rv (MOI 1:10). After infection, cells were treated with SQ109 (5 μM, 10 μM) for 24 hours, lysed, and plated for CFU counting. Results: SQ109 concentration-dependently reduced intracellular viable bacteria, confirming its ability to enhance macrophage killing of M.tb. [1] |
| In vivo | Methods: C57BL/6J mice were aerosol-inoculated with a low dose of M.tb H37Rv (110 CFU/lung). Starting on day 15 post-infection, SQ109 (10 mg/kg body weight) was administered via intraperitoneal injection daily until the euthanasia time points (days 22 and 35 post-infection). Results: SQ109 significantly reduced bacterial load in lungs and spleen. Lung histopathology revealed decreased inflammatory and necrotic lesions. [1] Methods: New Zealand White rabbits were infected with M.tb H37Rv to form humanized tuberculous granulomas with cellular margins and caseous necrosis cores. SQ109 was administered at 40 mg/kg daily for 7 consecutive days. Plasma, lung tissue, isolated cellular lesion areas, and caseous necrosis foci were collected for drug concentration measurement. Results: SQ109 accumulates extensively in lung tissue and areas of cellular lesions, with a penetration coefficient >1000. Passive diffusion is slow in caseous necrosis lesions, and drug concentrations are low, suggesting that several weeks of administration are required to achieve steady state.[2] |
| Synonyms | NSC 722041 |
| Molecular Weight | 330.55 |
| Formula | C22H38N2 |
| Cas No. | 502487-67-4 |
| Smiles | CC(C)=CCC\C(C)=C\CNCCNC1C2CC3CC(C2)CC1C3 |
| Relative Density. | 0.97 g/cm3 (Predicted) |
| Storage | Pure form: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 21 mg/mL (63.53 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (6.05 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density. | |||||||||||||||||||||||||||||||
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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