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
- Measuring pKa in synthetic chemistry to help select the best structures for development
- Ensuring good compound selection to reduce the risk of late stage failures
- Understanding the ionization state of a drug, how it varies with pH and its effect on absorption
- Learning how the pKa changes due to solvent interactions, partitioning, precipitation or binding
- Improving ADME predictions and evaluating how changes to the molecule can affect the logP for a desired application
- Learning about a molecule’s capacity for supersaturation
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.
Resources
Acidity constants of hydroxyl groups placed in several flavonoids: Two flavanones, two flavones and five flavonols
Trends in oral small-molecule drug discovery and product development based on product launches before and after the Rule of Five”
Advanced in vitro methods in generic drug product development
"Utilizing Pion's SiriusT3 Platform" Webinar
Applying Computational Predictions of Biorelevant Solubility Ratio Upon Self-Emulsifying Lipid-Based Formulations Dispersion to Predict Dose Number
SiriusT3 Product Brochure
Extended Instrument Shut Down for Sirius T3 Storage Guidelines
Diclofenac Prodrugs for Intra-articular Depot Injectables: In Vitro Hydrolysis and Species Variation
Comparison of Cinchona Catalysts Containing Ethyl or Vinyl or Ethynyl Group at Their Quinuclidine Ring
pKa and physchem property measurements for the pharmaceutical industry
WEBINAR: How pKa Values are used in the Pharmaceutical Industry
WEBINAR: Understanding and Measuring pKa
LogP as a tool in intramolecular hydrogen bond considerations
Effect of vinylpyrrolidone polymers on the solubility and supersaturation of drugs; a study using the Cheqsol method
Acid‐base titrations of proteins in small volumes
The impact of cosolvent on measured log P values
Determination of hydrogen bonding properties using logP
Surface tension and supersaturation
Measuring the isoelectric point of peptides by potentiometric titration
Solubility Measurement
Measuring Physiochemical Properties
WEBINAR: Measuring solubility - what’s best for you?
WEBINAR: Physicochemical Properties and their relation to ADMET
WEBINAR: How Cheqsol Works
WEBINAR: Investigating Supersaturation and Solubility Enhancement
WEBINAR: State of the art UV methods for measuring pKa
WEBINAR: Accessing hydrogen bond parameters and their application in drug discovery
WEBINAR: Log P- History, Measurement and Applications in Drug Development
Early pharmaceutical profiling to predict oral drug absorption: Current status and unmet needs
Novel N-methylsulfonamide and Retro-N-methylsulfonamide Derivatives as 17b-Hydroxysteroid Dehydrogenase Type 2 (17b-HSD2) Inhibitors with Good ADME-Related Physicochemical Parameters
Partial Protection Against Multiple RT-SHIV162P3 Vaginal Challenge of Rhesus Macaques by a Silicone Elastomer Vaginal Ring Releasing the NNRTI MC1220
Physicochemical investigation of the influence of saccharide-based parenteral formulation excipients on l-p-boronphenylalanine solubilisation for boron neutron capture therapy
Cyclopentane-1,3-dione: A Novel Isostere for the Carboxylic Acid Functional Group. Application to the Design of Potent Thromboxane (A2) Receptor Antagonists
The ‘‘GI dissolution’’ method: a low volume, in vitro apparatus for assessing the dissolution/precipitation behaviour of an active pharmaceutical ingredient under biorelevant conditions
Structural and thermodynamic analyses of alpha-L-fucosidase inhibitors
New ideas about the solubility of drugs
Assessment of distribution- pH profiles
Multiwavelength spectrophotometric determination of acid dissociation constants Part VI. Deconvolution of binary mixtures of ionizable compounds
Physicochemical characterization of sildenafil: Ionization, lipophilicity behaviour, and ionic-partition diagram studied by two-phase titration and electrochemistry
Ionization Constants and Ionization profiles
Measuring Physiochemical Properties 2
4‐case chart to classify supersaturation and precipitation behavior
Measuring pKa values in 2-propanol to gain process understanding
Ionization Constants of Isoniazid and Benzimidazole
pH-metric titration to characterize aci-nitro tautomerism
Effects of solubility enhancing excipients
Faster Dissolution Methods
Low Volume Dissolution Assays
The effect of dissolution media, torque and flow speed
Biphasic dissolution studies of Felodipine
Dissolution & precipitation studies of carbamazepine cocrystals with small scale assays
Dissolution in presence of lipid to mimic absorption
Dissolution Experiments in Lipid Layers
Small scale assays for studying dissolution of cocrystals
Small volume dissolution of a poorly soluble drug as solid dispersions
Solubility of drugs in the presence of excipients in lipid based formulations
Supersaturation & precipitation of ionizable drugs with cellulose polymers
Physicochemical Studies of Triclosan
Simulated Lung Fluid media
Solubility measurement by extrapolation
Solubilities of morphine analogs
Characteristics of Felodipine ‐ HPMCAS Solid Dispersions
Dissolution Performance of Inhaled Products in Simulated Lung Fluid
In-situ Solubility Measurements of Ionizable Drugs
Determination of Aqueous Solubility by Extrapolation
A low volume method for screening Plasdone® polymers
Assay Expert Flyer
AN410 Measuring the isoelectric point pf peptides by potentiometric titration
AN15 Determination of pKa Measurement or Prediction?
AN14 Using NaOH and NaCL instead of KOM and KCI
AN13 Measuring Solubility What’s Best for You?
AN12 Introduction to logP and logD Measurement Using SiriusT3
AN10 Measuring LogP of Samples that are Hard to Dissolve in Water and Octanol
AN09 The Determination of Solubility - Pion CheqSol Explained
AN08 Solubility and Supersaturation - A Brief Introduction
AN07 the Pion GI Dissolution Assay
AN06 The use of cosolvent pKa assays for poorly soluble compounds
AN05 Measurement of extreme pKas
AN04 Insights into BCS classification using Pion assays
AN03 Blank Titrations Using the SiriusT3
AN02 PKa measurements in 15 minutes - the SiriusT3 Fast UV pKa method
AN01 High quality measurements for small sample amounts
Pion SDi2 and Raman spectroscopy - study of diclofenac sodium salt
Behavior of Basic Compounds in the Presence of Plasdone Polymers
Determination of pKa values and Solubility pH Profiles of Selected ß blockers
Supersaturation in additives and GI fluids
Validation of titrimetric measurement of pKa, logP and solubility
The intrinsic solubility of indomethacin
Measuring the solubility of salts of basic drugs
Potentiometric techniques for measuring solubility at 37°C
Karl Box Sunrise Presentation
Determination of Polymer Effectiveness
Utilization of pH-Metric Titration
Consumables
2.5mL Plunger
T306034
0.5mL Plunger
T306033
T3 - Three Capillary Assembly
T306036(3)
T3 - Five Capillary Assembly
T306036(5)
T3 - Six Capillary Assembly
T306036(6)
SiriusT3 - Mini-electrode
T485024
T3 - Sample Vials - Pack of 1000
T304036
T3 - Sample Vials - Pack of 100
T304037
T3 - Sample Vial Caps - Pack of 100
T304038
Wash Vial - Pack of 2
T304041
Buffer Vial - Pack of 5
T304042
T3 - Extended Life Deuterium Lamp
T409004
48 well vial rack
T210046
Stainless Steel Vial Rack
T210049
Ultrasonic Bath Cover
T210050
PEEK Electrode Block Rev G
T210045
Electrode Block Skirt
T210051
Waste Bottle
T305119
Wash Water Bottle
T305120
250mL Bottle
T305083
500mL Bottle
T305084
250mL Machined Bottle Top
T305086
250mL Bottle Top Plate (1 hole)
T305089
T3 - pH7 Buffer
1402002
T3 - Neutral Linear Buffer
T1404007
T3 - Electrode Filling Solution - Pack of 2
1402012
Mini Stirrer Assembly MKII
T1015066
Mini Bubbler
T210047
Analytical Services
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