Celebrating 20 Years of Customer Service
Over the past decade, MicroSource has led the industry in the development of collections of bioactive substances in the search of new therapeutic agents.
There are many substances in the literature that have shown biological promise but never reached marketable status. Today's plethora of new assays based on the Human genome and advances in our understanding of biochemical processes have led us to gather a collection of these "under developed" entities and make them available for HTS discovery.
Our DISCOVER collection is comprised of 560 compounds that have shown biological potential in peer-reviewed publications but have never led to their development as drugs in human diseases. We offer these to you as a supplement to our drug collections to expand the scope of your inquiry.
US Drug Collection
An important collection of 1280 drugs that have reached clinical trial stages in the USA. Each compound has been assigned USAN or USP status and is included in the USP Dictionary (U.S. Pharmacopeia, 2012), the authorized list of established names for drugs in the USA. References
International Drug Collection
This collection comprises 320 drugs that are marketed in Europe and/or Asia but have not been introduced in the US. Such compounds have received INN, BAN and/or JAN designations, and are listed in the Index Nominum, the International Drug Directory. References
PHARMAKON 1600 is a unique collection of 1600 known drugs from US and International Pharmacopeia. Unlike competitive products, all compounds within the PHARMAKON 1600 Collection have reached clinical evaluation and not simply demonstrated biological activity experimentally. Most of the constituent drugs are still in the market. Data provided for each compound define its structure, CAS #, formula, molecular weight, biological profile and generic & market name. Literature references to use and toxicology are also included.
The term PHARMAKON is an ancient Greek term that refers to medicinal preparations that were used to alleviate a patient's symptoms and, on occasion, cure the disease. PHARMAKON also encompassed poisons that were believed to provide therapeutic benefit with judicious use. The term still reflects the character of today's medicines and a fitting title for this remarkable collection.
The NatProd Collection
Our natural product collection of 800 compounds is derived from commercial sources including our affiliate Gaia Chemical Corporation. All are fully characterized according to literature reports, and meet our criteria of a minimum of 95% purity. We select the compounds included in the NatProd Collection on the basis of structural and chemical class. At present approximately 75% of the collection encompasses: alkaloids (16%), flavanoids (12%), sterols/triterpenes (12%), diterpenes/sesquiterpenes (10%), benzophenones/chalcones/stilbenes (10%), limonoids/quassinoids (9%), and chromones/coumarins (6%).The remainder of the collection includesquinones/quinonemethides, benzofurans/benzopyrans, rotenoids/xanthones, carbohydrates, and benztropolones/depsides/depsidones, in descending order. References
The Killer Plates
Reference collection of 160 synthetic and natural toxic substances (plates A and B). An unprecedented opportunity to tease and test your assay. Inhibitors of DNA/RNA synthesis, cellular respiration, membrane integrity and much more. References
The Spectrum Collection
Now expanded to 2400 compounds, the components of the SPECTRUM Collection have been selected by medicinal chemists and biologists so as to provide a wide range of biological activities and structural diversity for screening programs with special emphasis on the de-novo assays emerging today. Such content provides the opportunity to evaluate drugs and biochemical tools with known biological profiles and, at the same time, explore the potential of novel structural and topographical diversity manifest in pure natural products. Each compound has a minimum of 95% purity unless otherwise specified.
The Drug Components (66%)
Drugs are defined according to the name designations as set forth in the USP Dictionary of USAN and International Drug Names (2012, US Pharmacopeia). Included are USP (US Pharmacopeia), USAN (US Adopted Name), INN (International Non-proprietary Name), BAN (British Approved Name), and JAN (Japanese Accepted Name) designations. Drugs that have been introduced in the US (1280 compounds with USAN/USP designations) predominate. Also included are 320 drugs that are limited in use to Europe (INN & BAN) and Japan (JAN). While most of these are off-patent, we have endeavored to include the more recent "blockbuster" drugs which are still covered by active patents in the United States. These, which constitute approximately 2% of the drugs in the Collection are isolated in our laboratory from the patent holder's or their assigned manufacturer's product. In this situation, patents rights have been extinguished, and the independent sale of the compound is without restriction. The use of such compounds, as purchased from MDSI by a customer, is similarly permitted for research purposes. No rights to any of these drugs or discoveries made with them are retained by MDSI or others. We do not place restrictions or invoke intellectual property issues in the use of our reference compounds.
Most of these drugs are synthetic or at least semi-synthetic in origin, although approximately 5% are naturally occurring. The pharmacological and toxicological profiles of these drugs have been defined and published. They serve to reflect the impact of their primary therapeutic activity in your assay system, but also to provide the opportunity of uncovering a previously unknown property that may lead to 'new use" development with supporting toxicological data.
The Natural Products (26%)
The remainder of the SPECTRUM collection includes 640 additional pure natural products which are derived from natural sources worldwide. Many of these are isolated and purified in our laboratories or those of our affiliates, Gaia Chemical Corporation and Planta Analytica LLC. These compounds are selected on the basis of chemical class and structural diversity.
Other Bioactive Components (8%)
Representatives of non-drug enzyme inhibitors, receptor blockers, membrane active compounds, and cellular toxins are provided in the SPECTRUM collection. Many of these compounds have either not reached development or been dropped for toxicological or other reasons. Also included are representatives of marketed pesticides and herbicides for comparative purposes. These diverse compounds are important assets in defining the scope of your assay and, once again, may reflect an unforeseen activity.