Hi everyone, I am dissolving Atrasentan (HY-15403) in DMSO, PEG 300, Tween 80, and saline, followed by mixing with ddH2O for oral administration. According to the literature, I plan to use this solution as the drinking water for the mice to continuously administer Atrasentan. Specifically, I added 1 mL of DMSO, 4 mL of PEG300, and 0.5 mL of Tween80 to 17 mg of Atrasentan and mixed it uniformly. Then, I added 4.5 mL of saline to make a total volume of 10 mL. After that, I added 990 mL of ddH2O to make a total volume of 1000 mL. All products used were new. The mice are on a high-fat diet and are model mice with elevated blood pressure. However, I have observed a white precipitate in the aqueous solution that does not dissolve despite heating and sonication. Is there any alternative method or solvent to improve the solubility of Atrasentan in this context? Thank you in advance!
Hello Janice, Atrasentan itself is not water soluble. You can first dissolve it directly in DMSO and then dilute it with drinking water to a final concentration of 100 mg/L, or use the Protocol 1 formulation for oral administration, which can dissolve up to 2.5 mg/mL (well above 0.017 mg/mL). Since you’re working with model mice, we recommend reducing the DMSO concentration to around 2%.
If you want to prepare 1000 mL drinking water with Atrasentan. First, dissolve 17 mg of Atrasentan in 20 mL of DMSO to prepare a clear stock solution (0.85 mg/mL). Next, add 400 mL of PEG300 and mix thoroughly until the solution is clear. Then, add 50 mL of Tween-80, mix well to ensure clarity, and finally add 530 mL of saline to reach a total volume of 1000 mL. The final working concentration will be 0.017 mg/mL. (Note: the drinking water with drug has to be freshly prepared every 1-2 days).
The answer to this question comes from MedChemExpress Technical Support.
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