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Aqueous Solubility

AW Amy Q. Wang
NH Natalie R. Hagen
EP Elias C. Padilha
MY Mengbi Yang
PS Pranav Shah
CC Catherine Z. Chen
WH Wenwei Huang
PT Pramod Terse
PS Philip Sanderson
WZ Wei Zheng
XX Xin Xu
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Kinetic aqueous solubility was determined at NCATS using Pion’s patented µSOL assay as described previously (Sun et al., 2019).

Equilibrium solubility was measured in pH 2.0, 5.0, 7.4 aqueous buffers as well as Simulated Gastric Fluid (SGF; pH 1.6), Fasted State Simulated Intestinal Fluid (FaSSIF; pH 6.5) and Fed State Simulated Intestinal Fluid (FeSSIF; pH 5.8). Briefly, >1 mg of GS-441524 powder was combined with 1 mL of buffer to make a >1 mg/mL mixture. Samples were shaken on a Thermomixer® overnight at room temperature and then passed through a 0.45 μm PTFE syringe filter. The filtrate was then sampled and diluted in a 1:1 mixture of buffer:ACN prior to analysis by UPLC-MS/MS.

Copyright and License information:  ©2022 Wang, Hagen, Padilha, Yang, Shah, Chen, Huang, Terse, Sanderson, Zheng and Xu.
This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) and the copyright owner(s) are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms.

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