Attachment 1 - Purchase Description.pdf

PURCHASE DESCRIPTION

Flash Chromatography System with Integrated ELSD Detector

STATEMENT OF NEED:

The National Institute on Drug Abuse Intramural Research Program requires a brand name or equal a flash chromatography system with integrated Evaporative light scattering detector (ELSD) for the real-time analysis of compounds designed and synthesized for the study and treatment of substance use disorders.

The most integral part of our medicinal chemistry program and especially organic synthesis is the ability to structurally characterize the novel molecules that are prepared in the Drug Design and Synthesis Section, Molecular Targets and Medications Discovery Branch (MTMDB). A critical tool for this characterization used by all our chemists in the laboratory is a flash chromatography with ELSD detector that provides data frequently needed for identification of target ligands on a daily basis. This system enables us to identify our peak of interest at the time of elution with the advantage of targeted fraction collection while maintaining excellent recovery and purity.

BACKGROUND INFORMATION AND OBJECTIVE:

The Drug Design and Synthesis Section (DDSS) major research direction is the elucidation of the structure and function of neurotransmitter systems in the mammalian central nervous system (CNS) in normal, drug-altered, and pathological states and the molecular mechanism of action of CNS active drugs.

Organic/medicinal chemistry is the foundation of the multidisciplinary approach utilized in these studies that require the rational design and chemical synthesis of novel agonists, antagonists, imaging agents, affinity ligands, and other drugs for applications. DDSS’ principal focus is the application of these techniques to study the mechanism of action of drugs and the development of medications for the treatment and prevention of drug abuse. The flash system with ELSD detector shall enable NIDA to identify compounds peak of interest at the time of elution with the advantage of targeted fraction collection while maintaining excellent recovery and purity. Additionally, the system will enable NIDA to efficiently and effectively continue synthesizing the necessary target compounds.

The ELSD component is a critical detection mode required in the flash system. In NIDA’s current system, the ELSD is ideally suited for drug discovery research conducted in DDSS.

1. NIDA’s research group synthesizes various types of molecules, including alkyl and PEG linkers that lack UV activity or have very weak UV activity. In addition, many of the compounds do not have ionizable groups and as such cannot be detected using UV and MS detection methods. ELSD enables detection of such compounds because it does not require that the compound of interest contain a chromophoric, fluorophoric, electroactive, or other type of functional group to provide a response.

2. The high sensitivity of the ELSD is another critical parameter. ELSD identifies analytes with uniform sensitivity regardless of their spectroscopic properties and it can provide quantitative information about essentially all components of the mixture, including inorganic impurities. Compounds synthesized in DDSS are evaluated in several in vitro and in vivo biological assays and purity is of highest importance as presence of contaminations can potentially have detrimental effects on the end results.

3.Purifications of polar, amine- functionalized or polyfunctional compounds are particularly challenging and often require using a) solvents that absorb UV light, such acetone and can compromise detection of the desired molecules, or b) separation modes with different polarities, for example normal-phase or reversed-phase. ELSD is the detector of choice in both cases as it does not rely on the presence of chromophores and is compatible with normal- and reversed-phase mode of separations.

4. The ELSD is integrated into NIDA’s current flash system and is very easy-to-operate, which is extremely important when users lacking experience or with limited experience must use the instrument routinely. More importantly, all experimental parameters of the ELSD are empirically determined, set and adjusted automatically depending on the separation mode in use. Thus, any user-related errors and potential loss of material are eliminated. The system also automatically shuts off the nitrogen gas.

5. Only an instrument with an integrated ELSD will fit the footprint available in the valuable fume hood space required of an instrument that uses flammable solvents and other chemicals to satisfy all personnel and infrastructure safety regulations.

GENERIC NAME OF PRODUCT:

Flash Chromatography System with integrated ELSD

SALIENT CHARACTERISTICS:

The Contractor shall provide the following brand name or equal items:

1. One (1) CombiFlash NextGen 300+ Automated Flash Chromatography System with integrated ELSD detector [Part No. 685250001], UV detector 200-400 nm with PeakTrak software control via 12" capacitive touchscreen. Flow rate range of 1-300mL/min. Maximum pressure limit of 300psi (20bar) Automated solid load injection valve. RFID rack and column read. Automatically loads column method information and writes back run information to the column. Automatically loads rack configuration. Active solvent level sensing One set of collection racks (quantity 2):

a. 18x150mm test tubes (Standard)

b. 234V - (150) 16x150mm test tubes (Standard)

2. One (1) ELSD for CombiFlash NextGen 300 and 300+ [Part No. 605257001]. To be installed in units when ordered with the NextGen. Installation cost to be added for field installations.

3. One (1) Installation and set-up.

The Contractor shall include warranty coverage on the subject equipment by Original Equipment Manufacturer (OEM) factory-trained, authorized technicians and providers of any required parts and software or proprietary diagnostic software and software enhancements must be OEM certified and compatible with the subject equipment. Troubleshooting will be available through phone technical service to reduce instrument downtime.

DELIVERY:

Delivery shall be made no later than 90 days after receipt of order (ARO) to the following locations:

Mariena Mattson

NIH/NIDA

9800 Medical Center Drive, Rm 239A Rockville, Maryland 20850 301-451-5064 mattsonm@nida.nih.gov

Delivery and installation and confirmed working operation of flash chromatography with ELSD system.

GOVERNMENT RESPONSIBILITIES

The government owns the scientific instrumentation. The field service technician shall be required to notify the POC from NIDA IRP for access to the subject equipment. Contractor shall provide installation, maintenance and repairs during regular Monday-Friday business hours, excluding Federal holidays. The systems shall be located in NIDA space in A building, second floor, 9800 Medical Center Drive, Rockville, MD 20850. Point of contact is Mariena Mattson, 301-451-5064.