Molecular Target for Screening: G-Protein-Coupled Receptors, ActiTarg-G
Filed under: Chemistry News, Compound Libraries, Compounds for HTS, New Products
Newark, DE. August, 2010 – Press Release – TimTec, LLC. – Molecular Target for Screening: G-Protein-Coupled Receptors, ActiTarg-G
G-Protein-Coupled Receptors are the largest gene families in the human genome and, rightfully so, have become the leading molecular target in 2008. In 2009 SBS April meeting in Lille, France, followed-up with screening trends report stating that “GPCRs are expected to replace protein kinases as the most common molecular target used by HTS laboratories.”
GPCRs are the largest family of cell surface receptors being integral to the number of cellular and physiological functions, including light sensing, smell, appetite control, insulin secretion, and blood pressure modulation. These receptors generally have a seven-membrane spanning alpha-helical topography, and while these receptors are similar in overall structure and function, they differ in key amino acid residues. The potential for this super family of receptors to reveal small molecule modulators of a significant biological function has been responsible for the focus of intense drug discovery efforts.
TimTec GPCR Ligands library is called ActiTarg-G. It currently counts 2,300 molecules available in various formatting options, and can be delivered in vials or in 96 or 384-well plates. ActiTarg-G is the set of diverse molecules that contain chemical lattices present in compounds reported in the technical or patent literature to possess GPCR-ligand properties.
Contact Information to schedule free consultation:
TimTec LLC
Harmony Business Park A-301
Newark DE 19711
Tel 302 292 8500
Fax 302 292 8520
Web: http://www.timtec.net/news/timtec-news/actitarg-g-gpcr-ligandshtml.html
About TimTec
TimTec LLC is a privately held company located in Newark Delaware, USA. It was founded in 1995 and began its work in the areas of acquisition and distribution of synthetic organic and natural compounds and collections, custom synthesis, and laboratory equipment to become a full service partner for drug discovery. TimTec has established a global network of thousands of scientists from research centers around the world. International customers include major pharmaceutical, biotech, agricultural, and educational companies and institutions, which use TimTec products for research and development programs.
FEP Multi-Channel Distillation Column Packing
Solvent recycling saves money and is good for the environment. Using our PFE column packing, solvents can be efficiently recovered and reused, reducing environmental burden and spent solvent disposal costs. With the proper column height, solvents can be restored to their original purity or better.
The packing’s unique geometric shape was developed in our chemical R&D laboratories for the purification of deuterated solvents and solvent recovery. Liquid does not pool irregardless of packing orientation. The surface is completely inert to polar and non-polar solvents, acids and bases, thereby eliminating any possible metal, organo-metalic, or monomer contamination as when using other packing materials. Due to the inert nature of PFE, cleaning and drying the packing for later use is easy and straight forward.
As an example of its distillation efficiency, we were able to produce 99.9% atom D2O from water using regular types of distillation columns and receivers. We have also distilled organic solvents to 99.99% purity and have recycled these for our own use. If you are interested in solvent recovery, whether for HPLC, HPLC-NMR, wet chemistry or other use, Norell’s PFE column packing is the leading product of choice.
http://www.nmrtubes.com/
Nine U.S. Health Research Centers to Receive $255 Million
Nine health research centers have received funds to develop ways to reduce the time it takes for clinical research to become treatments for patients. The funds were awarded as part of the Clinical and Translational Science Awards (CTSA) program which is led by the National Center for Research Resources (NCRR), part of the National Institutes of Health.
“A critical goal of biomedical research is to transform discoveries into preventions, treatments, and cures,” said NIH Director Francis S. Collins, M.D., Ph.D. “By working together, CTSAs are removing barriers to research, training new generations of clinical and laboratory research teams, and providing them with the equipment and resources they need.”
Now in its fourth year, the CTSA consortium has generated resources that transform the research and training environment to enhance the efficiency and quality of clinical and translational research. Examples include a Web-based national recruitment registry that connects researchers with volunteers interested in participating in clinical studies, establishing public-private partnerships, and a portal that connects researchers with potential investigational drugs that may be useful in new ways.
The 2010 CTSAs expand consortium representation in new areas including New Mexico, Virginia and the District of Columbia, growing the consortium to 55 member institutions. The nine new institutions are:
Children’s National Medical Center, Washington, D.C.
Georgetown University with Howard University, Washington, D.C.
Medical College of Wisconsin, Milwaukee
University of California, Irvine
University of California, San Diego
University of Massachusetts, Worcester
University of New Mexico Health Sciences Center, Albuquerque
University of Southern California, Los Angeles
Virginia Commonwealth University, Richmond
View descriptions of these CTSA awardees at www.ncrr.nih.gov/ctsa2010.
“The nine institutions that have received CTSAs this year extend the geographic reach of the consortium and bring additional talent and expertise in such areas as children’s health, outreach to underrepresented communities, and systems to share research information,” said NCRR Director Barbara Alving, M.D.
The CTSA consortium now includes awardees in 28 states and the District of Columbia. When the program is fully implemented in 2011, it will support approximately 60 CTSAs across the nation.
A sixth and final funding opportunity announcement for CTSAs is available, calling for the next round of applications to be submitted by Oct. 14, 2010, with the awards expected in July 2011. For more information about this funding announcement, see www.ncrr.nih.gov/crfunding.
For more information about the CTSA program, visit www.ncrr.nih.gov/ctsa. The CTSA consortium website, which provides information on the consortium, current members and new grantees, can be accessed at www.CTSAweb.org.
The National Center for Research Resources (NCRR), a part of NIH, provides laboratory scientists and clinical researchers with the resources and training they need to understand, detect, treat and prevent a wide range of diseases. NCRR supports all aspects of translational and clinical research, connecting researchers, patients and communities across the nation. For more information, visit www.ncrr.nih.gov.
The National Institutes of Health (NIH) — The Nation’s Medical Research Agency — includes 27 Institutes and Centers and is a component of the U.S. Department of Health and Human Services. It is the primary federal agency for conducting and supporting basic, clinical and translational medical research, and it investigates the causes, treatments, and cures for both common and rare diseases. For more information about NIH and its programs, visit www.nih.gov.
Alfa Aesar Now Offers Homopiperazines
Alfa Aesar, a Johnson Matthey Company, has entered into a distribution agreement with Tosoh Organic Chemical Co. Ltd., a recognized world leader in the development and production of unique organic chemical intermediates.
Alfa Aesar is the sole distributor of research and development quantities of substituted homopiperazine products from Tosoh. Substituted homopiperazines have shown promise in drug discovery as intermediates in the production of compounds suitable for the generation of diverse combinatorial libraries. The select products are in stock and are available for immediate shipment. This technology can be applied to a wide variety of related materials; if there are additional compounds of interest please feel free to contact Alfa Aesar for further discussion.
Homopiperazines
- H51685
1-(2-Methylphenyl)homopiperazine monohydrochloride, 98% - H51686
1-(3-Fluorophenyl)homopiperazine monohydrochloride, 98% - H51687
1-(4-tert-Butoxyphenyl)homopiperazine monohydrochloride, 98% - H51700
1-(3-Methylphenyl)homopiperazine monohydrochloride, 98% - H51701
1-(4-Fluorophenyl)homopiperazine dihydrochloride, 98% - H51702
1-(4-tert-Butylphenyl)homopiperazine dihydrochloride, 98% - H51703
1-(4-Methoxyphenyl)homopiperazine monohydrochloride, 98% - H51750
1-(4-Methylphenyl)homopiperazine monohydrochloride, 98% - H51751
1-(3-Methoxyphenyl)homopiperazine monohydrochloride, 98% - H51752
1-(3-tert-Butoxyphenyl)homopiperazine monohydrochloride, 98%
TimTec Contract Research Services
TimTec brings 15 years of expertise in organic chemistry design and supply for drug discovery closer to your supplemental bench-top requirements by launching The Organic Synthesis and Medicinal Chemistry Contract Research Services Division. TimTec scientists have a proven track record of providing high quality services and showing outstanding integrity to their clients.
TimTec remains flexible in delivering practical chemistry solutions molded to custom research requirements and budgets. All Contract Research Services are delivered with an emphasis on speed, real-time feedback, ongoing communication, superior compound quality, and the protection of our clients’ knowledge resources and interests. We are dedicated to providing these services at exceptionally competitive prices.
The Head of Contract Research Services has over 20 years of research experience in the US pharmaceutical industry as a hands-on medicinal chemist and project Team Leader at large companies and smaller, start-up operations. We are keenly aware of all the intricate details and chemistry challenges that go into bench-top research before a qualified lead molecule emerges. Your TimTec contract research team consists of experienced, bench level scientists who have access to state of the art synthesis, analytical and quality control facilities.
TimTec Contract Research Services Start with:
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Flexible Contracts
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Program Management
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State of the Art Facilities
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Structure-Activity Relationship Evaluation
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Lead Optimization
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Property Optimization for ADME and PK
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Metabolite Synthesis
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Enabling Technologies – Parallel synthesis, multistep synthesis, analytical chemistry
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Mg to Kg Capacity
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Compound Distribution – Solid or solution, vials or plates
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Patent Application Preparation Assistance
Supplemental Services and Products:
HTS compounds and compound collections – ActiMol Line of products
Neuronetrix’ COGNISION™ System
Alzheimer’s disease is a chronic neurodegenerative disease of the brain which afflicts roughly 5 million individuals in the United States. Approximately 10% of those over 65 and 50% of those over 85 will die as a result of Alzheimer’s disease.
Even with several therapies available to treat Alzheimer’s disease, there still is a significant gap between the onset of the disease and point at which treatment actually begins. This treatment gap is directly tied to the challenges in diagnosing the disease early, before the significant loss of memory, cognition, and activities of daily living. Patients, doctors, caregivers, and the pharmaceutical industry, are looking for and demanding a solution to this problem.
Neuronetrix’ COGNISION™ System will, for the first time, directly detect the abnormal cognitive effects of Alzheimer’s disease! This will facilitate an earlier and more accurate diagnosis than is currently available. Physicians will use the COGNISION™ test to determine which patients would benefit from the available drug treatments. The system can also be used to monitor the efficacy of the prescribed therapy.
With the aging of America and the proliferation of new Alzheimer’s therapies, the market for Alzheimer’s screening could approach several billion dollars per year in the United States alone.
Following the validation of the COGNISION™ System for Alzheimer’s disease, Neuronetrix will expand into other neurodiagnostic markets such as ADHD, dyslexia, and depression.
http://www.neuronetrix.com/
Hebei Baocheng Chemical Co
Hebei Baocheng Chemical Co is a manufacturer and exporter of chrome oxide green ,chromic acid sodium bichromate etc chromium chemical in China,consist of five factorys,have been in this field for 30 years, main products including:chrome oxide green,fused chorme, chrome yellow,chromic acid,sodium bichromate,pottassium bichromate.
Annual production of chrome oxide green is 6,000 MT, chromic acid 4000 MT,sodium bichromate 4000 MT,chrome yellow 4000M/T.
- Chrome oxide green
- Chromic acid
- Sodium bichromate
- Potassium bichromate
- Chome yellow
- Fused chrome
http://www.bcchrome.com
Lipinski Rule-of-Five
Lipinski’s rule-of-five analysis
Christopher Lipinski’s rule-of-five analysis helped to raise awareness about properties and structural features that make molecules more or less drug-like. The guidelines were quickly adopted by the pharmaceutical industry as it helped apply ADME considerations early in preclinical development and could help avoid costly late-stage preclinical and clinical failures. The guidelines predict that poor absorption or permeation of a orally administered compound are more likely if the compound meets the following criteria:
* Molecular mass greater than 500 Da
* High lipophilicity (expressed as cLogP greater than 5)
* More than 5 hydrogen bond donors
* More than 10 hydrogen bond acceptors
Biological Safety Cabinets
By Angelo DePalma
From Lab Product News
Biological safety cabinets (BSCs) are specialized work areas that provide protection to users/operators and/or samples. BSCs are categorized as Class I, Class II or Class III, depending on their construction, airflow characteristics and exhaust systems. These classifications are based on each BSC’s suitability for samples at various biosafety levels. Class I and Class II cabinets handle Biosafety Levels 1, 2 and 3 (low to moderate risk), while Class III BSCs are intended for use with Biosafety Level 4 agents (high risk).
BSCs are distinct from other safety enclosures. Laboratory fume hoods pull air over the work item and out into the environment through a vent, whereas controlled atmosphere glove boxes are completely enclosed, protecting both users and samples through an airtight barrier. A distinguishing component of BSCs is their use of high-efficiency particle air (HEPA) filters, which scrub effluent between 99.5 percent and 99.99 percent of airborne particles, or at least 99.97 percent of particles larger than 3 microns.
Class distinctions
Class I BSCs protect personnel and the environment only. Samples are vulnerable because workspace air is swept over them before filtration and venting. Class II cabinets represent a broad category, with varying capabilities that are further subdivided into categories A1, A2, B1 and B2. The main differentiator between Class I and Class II BSCs is that Class II cabinets employ a HEPA-filtered, vertical, unidirectional airflow within the work area. Class III BSCs, which provide the highest level of protection to both workers and samples, are reserved for highly contagious or virulent biological samples.
Class II A2 cabinets are by far the most common BSCs in use today, comprising about 95 percent of installations, according to David Phillips, technical applications specialist at Thermo Scientific (Asheville, N.C.).
Class II cabinets have open fronts. Workers are protected by the steady vertical airflow. An ongoing controversy for specifying certain Class II cabinet types involves NSF Standard 49, which states that Class II A2 and B2 cabinets are designed to handle “minute” amounts of toxic chemicals and radionuclides. “But nobody has defined the term ‘minute’ quantitatively,” admits Phillips, who works on the NSF joint committee that determines BSC specifications.
To satisfy whatever that requirement might be, and to err on the side of caution, most laboratories automatically specify the use of Class II B2 cabinets, which Phillips describes as “complex, infrastructure sensitive and 10 times trickier to run” than Class II A2 cabinets. “A lot of people get stuck with B2s, but half of them should never have been installed. Users would be much better served by canopied A2 cabinets.”
Jim Hunter, senior project engineer at Labconco (Kansas City, Mo.), suggests using B-type cabinets in situations where workers are consistently working with volatile toxic agents, isotopes or anticancer drugs that you don’t want coming back into the lab. Otherwise, the acquisition and operating costs are simply not worth it. “B cabinets cost a lot of money and use a lot of energy. Unfortunately, architects assume a B cabinet is always better because it’s more expensive or because the letter ‘B’ comes after ‘A’ in the alphabet. All too often they simply override a customer’s decision on which type of cabinet to purchase,” says Hunter.
As a former certifier of BSCs, Phillips has a unique perspective on the evolution of these cabinets. In the past, he says, cabinets were commodities that barely differed as one considered the product offerings of numerous vendors. “They basically all looked like battleships,” he says. Beginning in the 1990s, cabinets began incorporating ergonomic designs that allowed operators to move forward and backward in comfort. Enclosures became brighter and air-handling systems quieter (through the adoption of DC motors and computer-controlled airflow compensation). “Cabinets evolved from being cookie- cutter-type products to having more choices and options. It’s a really fun time to be in this industry,” says Phillips.
One improvement affecting both operating costs and the environment is energy consumption. Older-model BSCs were energy hogs, but today’s units are downright miserly. Phillips recalls an event at the University of Michigan, where one of his Thermo Fisher colleagues was accused of low-balling the power consumption of a Thermo Fisher BSC. The assembled scientists were forced to eat their words after they tested the product and measured its energy usage. The result was a paper you can find at http:// bit.ly/N9bwz.
Environmental concerns have become a huge factor in BSC purchases, according to John Peters, assistant marketing director at Nuaire (Plymouth, Minn.). “Customers look for energy efficiency as well as total cost of ownership, the life of HEPA filters and the types of motors used to drive the air handlers,” he explains. Unlike many other laboratory products, purchasers of BSCs must perform their own due diligence, as no third-party organizations provide energyefficiency ratings for cabinets.
CambridgeSoft’s Annual Conference and User Meeting on August 24th & 25th at the World Trade Center in Boston.
The 2010 CambridgeSoft’s Conference and User Meeting will being held in Boston on August 24 & 25, 2010.
This event will highlight keynote addresses from leading pharmaceutical companies, present real-world applications of our scientific software solutions, and update attendees with information on some of our newest products and services.
Please mark your calendars for this exciting event. Admission is free for qualified industry professionals, but space is limited, so please register early. The timing of the Conference and User Meeting coincides with the ACS Fall meeting in Boston, so this is a great opportunity to attend both events while in town.
Location:
Boston, USA
World Trade Center
When : August 24, 2010 - August 25, 2010
Event Description:
http://www.cambridgesoft.com/seminars/?eventid=278