Bindley Bioscience Center

Libraries

The LOPAC1280 Sigma library includes the latest, drug-like molecules in the fields of cell signaling and neuroscience:

  • Apoptosis
  • G proteins & cyclic nucleotides
  • Gene regulation & expression
  • Ion channels
  • Lipid signaling
  • Multi-drug resistance
  • Neurotransmission
  • Phosphorylation

The following link will allow a researcher to explore the library by application areas that drill down by class, selectivity, and action.  Researchers can also search for a compound by name or product number to view structures for all library components:

http://www.sigmaaldrich.com/Area_of_Interest/Chemistry/Drug_Discovery/
Validation_Libraries/LOPAC1280home.html

Note: The following text (or part of it) may be hidden.  Click on the link, LOPAC1280  (Library of Pharmacologically Active Compounds), to find a collection of high quality, innovative molecules that span a broad range of cell signaling and neuroscience areas.

The library is most commonly used to validate new drug discovery assays and characterize orphan receptors. All of the compounds are Sigma-RBI compounds that are held to the same quality standards that any Sigma-RBI product would be. Additionally, the catalog number for each compound is provided with the set to facilitate re-supply when necessary.

The complexion of the LOPAC1280 library reflects the most commonly screened targets in the drug discovery community. For example, G protein-coupled receptors (GPCRs) are the target for 60% of the therapeutics currently on the market. The sequencing of the human genome has identified 1000-2000 putative GPCRs.  Thus, GPCRs represent the most aggressively pursued targets and molecules that interact with GPCRs and comprise over 50% of the compounds in LOPAC1280.  The fact that ligands are known for only 200 GPCRs underscores the importance of orphan-receptor characterization projects.
Screening with proven pharmacological tools can provide new information based on relevant and diverse structures.  LOPAC1280 contains marketed drugs, failed development candidates, and “gold standards” that have well-characterized activities. These compounds are the result of lead optimization efforts and thus possess a great deal of value, having been rationally designed by structure-activity relationship (SAR) studies. Not only are successfully marketed drugs like fluoxetine and loratadine valuable for their activities, they offer a standard against which next-generation drugs can be measured in an effort to understand why candidates fail and, more importantly, why some candidates succeed.

Reagents

LOPAC1280 contains 1,280 pharmacologically active Sigma-RBI compounds arrayed in 96-well format. Each compound is supplied as 0.25 ml at 10 mM in DMSO (dimethylsulfoxide). The first and last columns of each rack are left empty to facilitate the use of controls. The resulting format is 16 racks containing 80 compounds per rack. Please refer to the rack map provided on the CD-ROM included with the set.

Precautions and Disclaimer

This product is for laboratory research use only. Please consult Material Safety Data Sheets for the set or individual components to assess handling recommendations before working with this material.

Preparation Instructions

Compound solubility in DMSO is not uniform. Be careful to re-suspend compounds that may settle prior to transfer.

Storage/Stability

LOPAC1280 should be stored at –20 °C to be protected from moisture and light.  Avoid repeated freeze/thaw cycles by producing working replicates.

Product Profile

Detailed information including compound names, well locations, structures and pharmacological activities can be found on the CD-ROM included with the set.

References
  1. Darvas, F. et al., ‘Estimation of stability and shelf life for compounds, libraries and repositories in combination with systematic discovery of new rearrangement pathways.’ In: Handbook of Combinatorial Chemistry (Eds. Nicolaou, K., Hanko, R. and Hartwig, W.) pp. 806-828, Wiley-VCH.

Contact

Address
Purdue University
Bindley Bioscience Center
Integrated Screening Technologies
BIND-Room 222
1203 West State Street
West Lafayette, IN 47907-2057
(765) 496-2869

Larisa Avramova
Ph.D. Research Scientist