SiriusT3
Pion’s SiriusT3 is a fully automated instrument designed for compound screening and preparing detailed PhysChem profiles.
The Sirius lets you use Pion’s proprietary CheqSol method to accurately determine the kinetic and intrinsic solubilities of ionizable compounds. It generates detailed information about the extent and duration of supersaturation and a pH-solubility profile from a single, highly automated assay which takes less than 2 hours.
‘SiriusT3 is the Gold Standard.’
Overview
The SiriusT3 is an essential tool for analyzing pure single-component organic chemicals and their salts. It measures pKa, logP, logD and solubility of ionizable drugs and small molecules, needing only very small amounts of sample. It is widely used in industrial and university labs, CROs and Pharma to support drug discovery research.
Customers describe the SiriusT3 as ‘integral’ for the physicochemical characterization of compounds and ‘a pre-requisite for DMPK studies’. Others praise how it ‘integrates perfectly’ into analytical workflow and how it can ‘aid in the selection of compounds to move forward into further PK testing’.
Applications
The SiriusT3 supports a range of tasks across early stage compound screening, physchem characteriza-tion and pre-formulation. These include:
✓ Determining intrinsic solubility
✓ Ensuring good compound selection to reduce the risk of late stage failures
✓ Learning how the pKa changes due to solvent interactions, partitioning, precipitation or binding
✓ Learning about a molecule’s capacity for supersaturation
✓ Measuring pKa in synthetic chemistry to help select the best structures for development
✓ Understanding the ionization state of a drug, how it varies with pH and its effect on absorption
✓ Improving ADME predictions and evaluating how changes to the molecule can affect the logP for a desired application
Features
Accuracy
The Pion pH-metric method provides independent confirmation that ionization has occurred and also helps characterize acidic and basic groups, in addition to logP and solubility. This eliminates the need for time-consuming shake-flask style experiments in multiple pH buffers.
LogP can be potentiometrically determined and logD vs. pH can be accurately derived from measured logP and pKa data. Likewise, equilibrium solubility vs pH can be derived from potentiometrically de-termined intrinsic solubility and pKa data. Partitioning behavior between water and octanol, toluene, dodecane and with other solvents can also be studied, along with the effects of excipients and co-solvents on solubility. The instrument comes with built-in methods for measuring compounds of high, medium and low logP, and for determining solubility of samples with differing precipitation behavior
Speed
With the SiriusT3, you can determine pKa values to the highest accuracy available commercially, with results in 15 minutes by Fast UV for most samples. It uses the UV-metric method for pKas below 2 and above 12; cosolvent methods for poorly soluble samples; pH-metric assays for samples without UV activity. Sample requirement: UV, 10 μg; pH-metric, 1 mg.
Simplicity
Many assays work with standard templates. Templates are supplied for all supported assays, including a 1-2-3 template for setting up co-solvent pKa assays. You can also save customized templates if re-quired.
Efficiency
The SiriusT3 makes measurements using small amounts of sample. Assays are performed in solution, 1 - 3 mL. Solutions are prepared in vials via automated dispensers and temperature-controlled be-tween 12 - 70°C..A built-in ultra-sonic bath helps to dissolve poorly soluble compounds. In addition, by running clean-up assays, you can ensure that the SiriusT3 is always ‘ready to go’.
Robotics
SiriusT3 has a fully automated X and Y axis on a titrator module probe arm, which is fully equipped for automatic reagent delivery, stirring, spectra collection, pH measurement and temperature control. This allows you to run complicated assays that could be challenging to set up manually.
Automation
The optional autoloader improves convenience and high throughput capabilities as experiments can be run unattended.