MODIFICATION
68 -- TRH AGONIST
- Notice Date
- 6/24/2014
- Notice Type
- Modification/Amendment
- NAICS
- 541711
— Research and Development in Biotechnology
- Contracting Office
- Department of Health and Human Services, National Institutes of Health, Nat'l Institute of Diabetes, Digestive, & Kidney Diseases, 2 Democracy Plaza, Suite 700W, 6707 Democracy Blvd., MSC 5455, Bethesda, Maryland, 20892-5455
- ZIP Code
- 20892-5455
- Solicitation Number
- NIHLM2014174
- Archive Date
- 7/24/2014
- Point of Contact
- V. Lynn Griffin, Fax: 301-480-8501, MAXWELL KIMPSON,
- E-Mail Address
-
griffinv@mail.nih.gov, Max.Kimpson@nih.gov
(griffinv@mail.nih.gov, Max.Kimpson@nih.gov)
- Small Business Set-Aside
- N/A
- Description
- MODIFICATION: TO CORRECT SOLICITATION NUMBER(S) IN TEXT. This is a combined synopsis/solicitation for commercial items prepared in accordance with the format in FAR 12.6 as supplemented with additional information included in this notice. This announcement constitutes the only solicitation and a separate written solicitation will not be issued. This solicitation number is NIHLM2014174 and is issued as a Request for Quotation (RFQ). The solicitation /contract will include all applicable provisions and clauses in effect through Federal Acquisition Circular 2005-73. The North American Industry Classification (NAICS) Code is 541711 with a size standard of 500 employees. This acquisition is being conducted using Simplified Acquisition Procedures in accordance with FAR Part 13. The National Institutes of Health (NIH), National Institute of Digestive, Diabetes & Kidney Diseases (NIDDK) has a requirement to procure TRH agonist. Many studies have linked TRH and TRH receptor to psychiatric disorders. For example, individuals with major depression exhibit a blunted thyrotropin (thyroid-stimulating hormone, TSH) response to TRH and absence of the nocturnal TSH surge, and decreased TRH gene expression was observed in the hypothalamus of depressed patients. TRH and TRHR in the limbic system and cortex are believed to mediate the endogenous and exogenous effects ofTRH on affect, mood and arousal but it has been notoriously difficult to assign specific functions and behaviors to extrahypothalamic TRH. Drug-like agonists for the TRH receptor that are metabolically stable and able to cross the blood-brain barrier might serve as probes to elucidate the roles of TRH receptors in the brains in animal models and might be valuable as lead compounds for the development of drugs to treat patients with several central nervous system (CNS) disorders and cancer-related fatigue. It is important to note that there are no known nonpeptidic agonists ofTRHR. The specific goal of this project is to discover/develop agonists for the TRH receptor. Chemical modifications of these compounds will be guided by computational docking of compounds into the binding pocket of a TRH receptor homology model. NIDDK/NIH has requested this procurement to develop a molecular ("homology") model of the thyrotropin-releasing hormone (TRH) receptor, use the model to rationally design "drug-like" ligands that bind to and activate the TRH receptor and then to chemically synthesize the ligands. This will be an iterative process in which a batch of ligands will be designed and synthesized then tested in a NIDDK laboratory and then based on the results of the tests another round of design, synthesis and testing will be pursued, etc. The purpose will be to develop a high affinity and potency agonist for the TRH receptor that may be a lead drug to treat humans with central nervous system disorders and cancer-related fatigue. There is no prior work in this area. It is noteworthy that a number of pharmaceutical companies have synthesized thousands of analogs of TRH but although they are active in vitro they are virtually ineffective when tested in animal models because of their rapid degradation in blood and their inability to penetrate the blood-brain barrier. A drug-like TRH receptor agonist may have a much longer halfllfe In blood and ability to penetrate the blood-brain barrier. NIDDK has requested Hit-to- Lead optimization of compound 18 for TRH agonist activity. The process will involve, molecular modeling, purchase of desired compounds and synthesis of new compounds to Improve TRH agonist activity. Contractor shall establish an SAR and exploration of novel intellectual property (IP) positions. Contractor shall work closely with NIDDK scientists and will include results of their biological tests in designing new sets of compounds. Project Timeline : This Is an Integrated project and shall require 6 months. Deliverables : a. Molecular modeling study b. Design of new compounds c. Procurement of about 25 commercially available compounds d. Synthesis of about 20 new compounds with > 95% purity in 20 mg quantity e. Intellectual Property (IP) search f. Project report Molecular Modeling : The molecular docking studies of the compound 18 at TRHR will be conducted sets of compounds will be designed and their drug like properties will be calculated in silica. After testing the new compounds by client, the model will be refined and next set of compound will be designed. Purchase of commercially available compounds : The compounds designed using molecular modeling will be checked for their availability from commercial source. The commercially available compounds will be purchased and shall be provide to the NIDDK. Synthesis of new compounds : The compounds designed based on molecular that are not commercially available will be synthesized 20 mg in quantity with> 95% purity and structure analysis by NMR and LC/MS. The offeror must include a completed copy of the following provisions: 1) FAR Clause 52.212-1 Instructions to Offerors - Commercial items; 2) FAR Clause 52.212-2, Evaluation - Commercial Items. As stated in FAR Clause 52.212-2 (a) The Government will award a contract resulting from this solicitation to the responsible offeror whose offer conforming to the solicitation will be advantageous to the Government, price and other factors considered. The following factors will be used equally to evaluate offers: Technical Evaluation, Price, and Past Performance. Note: Past Performance Information: Vendors must submit a listing of the most recent contracts/awards (minimum of 3) which demonstrate similar work in nature to this Solicitation. Contracts/awards may include those entered with the Federal Government, state and local governments and commercial concerns. Include the following information for each contract or subcontract: 1. Name of Contracting Organization 2. Contract Number (for subcontracts provide the prime contract number and the subcontract number) 3. Contract Type 4. Total Contract Value 5. Description of Requirement 6. Contracting Officer's Name and Telephone Number 7. Program Manager's Name and Telephone Number 3) FAR Clause 52.212-3, Offeror Representations and Certifications - Commercial Items; 4) FAR Clause 52.212-4, Contract Terms and Conditions - Commercial Items; 5) FAR Clause 52-212-5, Contract Terms and Conditions Required to Implement Statutes or Executive Orders - Commercial Items - Deviation for Simplified Acquisitions. The Dun and Bradstreet Number (DUNS), the Taxpayer Identification Number (TIN) and the certification of business size shall be included. The clauses are available in full text at http://www.arnet.gov/far. PLEASE NOTE: In order to receive an award, contractor must be registered and have valid certification in the System For Award Management (SAM) http://www.sam.gov Interested vendors capable of providing the Government with the items specified in this synopsis should submit their quotation to the below address. Quotations will be due fifteen (15) calendar days from the publication date of this synopsis July 9, 2014 at 11:00 a.m. EST. Offersors shall provide an original and two copies of your quotation. The quotation must reference Solicitation number NIHLM2014174. All responsible sources may submit a quotation, which if timely received, shall be considered by the agency. Quotations must be submitted in writing to the National Institutes of Health, National Library of Medicine, 6707 Democracy Blvd., II Democracy Plaza, Suite 700W, Bethesda, Maryland 20892, Attention: V. Lynn Griffin. Faxed copies will not be accepted.
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- SN03404521-W 20140626/140625022104-7c35d73acc1feb088c3157828cd24cfd (fbodaily.com)
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