D1 PD 060721.pdf

Purchase Description

Name of Item or Project Title:

PathHunter detection kit (PN 93-0001XL)

Statement of Need and Purpose:

The National Center for Advancing Translational Sciences (NCATS), Division of Pre-Clinical

Innovation (DPI), Early Translation Branch (ETB) has a requirement for a PathHunter detection kit (PN 93-0001XL) to enable high-throughput screening of a pain-related G protein coupled receptors (GPCRs) target, e.g., GALR1 and GPR151. NCATS has a need to detect the agonists or antagonists of those pain-related GPCRs with this kit which will also be used in several other NCATS drug targets of interest, e.g., EPO receptor.

Background Information and Objective:

The National Center for Advancing Translational Sciences (NCATS) is a part of the National

Institutes of Health (NIH), which mission it is to catalyze the generation of innovative methods and technologies that will enhance the development, testing and implementation of diagnostics and therapeutics across a wide range of human diseases and conditions.

As a part of HEAL (Helping to End Addiction Long-term) Initiative launched by NIH, NCATS is currently pursuing screening of new targets of Pain and Addiction. GPR151 is the new targets for pain and addiction and NCATS would like to discover small molecule modulators against this receptor.

To fulfill this goal, NCATS has developed a high-throughput screening (HTS) of GPR151. This

HTS amenable functional assays utilize “GPR151 beta-Arrestin cell line” generated from

Eurofins DiscoverX company, which have high expression of GPR151 on the cell membrane.

We have fully validated this assay and shown that upon GPR151 activation, this assay can generate specific luminescent signal and thus will be useful for screening GPR151 specific agonist.

The PathHunter detection kit is a crucial reagent in conducting primary drug screen in search for GPR151 modulators to fulfill the goal of HEAL initiative. The PathHunter detection kit will also be a useful tool in the secondary characterization of several other HEAL drug targets of interest, and so meets several stated needs.

Generic Name of Product:

Detection reagent detection kit

Purchase Description:

One (1) PathHunter detection kit, Part Number (PN) 93-0001XL including shipping to NCATS

Salient Characteristics:

The salient physical, functional, or performance characteristics that “equal” products must meet are as follows:

• The detection reagent need to be compatible with PathHunter Cell Lines to generate a chemiluminescent signal upon receptor stimulation;

• The kit should have enough reagent for a minimum of 500X 384 well plate detection

Purchase Description

• Shipping and Handling.

Quantity:

One (1) PathHunter detection kit (PN 93-0001XL)

Delivery:

The delivery shall be made to NCATS four (4) weeks after receipt of order (ARO), at the following location:

NCATS/NIH

9800 Medical Center Dr

Rockville, MD 20850