Delving into the Latest Updates on TUG-2015 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

FFAR3

Mechanism

FFAR3 modulators(free fatty acid receptor 3 modulators)

Therapeutic Areas

Endocrinology and Metabolic DiseaseOther Diseases

Active Indication

InflammationMetabolic Diseases

Inactive Indication-

Originator Organization

IT-Universitetet I København

Active Organization

University of Glasgow

University of Southern Denmark

IT-Universitetet I København

Inactive Organization-

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

Free fatty acid receptor 3 (FFA3, previously GPR41) is activated by short-chain fatty acids, mediates health effects of the gut microbiota, and is a therapeutic target for metabolic and inflammatory diseases. The shortage of well-characterized tool compounds has however impeded progress. Herein, we report structure-activity relationship of an allosteric modulator series and characterization of physicochemical and pharmacokinetic properties of selected compounds, including previous and new tools. Two representatives, 57 (TUG-1907) and 63 (TUG-2015), showed improved solubility and preserved potency. Of these, 57, with EC₅₀ = 145 nM and a solubility of 33 μM, showed high clearance in vivo but is a preferred tool in vitro. In contrast, 63, with EC₅₀ = 162 nM and a solubility of 9 μM, showed lower clearance and seems better suited for in vivo studies. Using 57, we demonstrate for the first time that FFA3 activation leads to calcium mobilization in murine dorsal root ganglia.

100 Deals associated with TUG-2015

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Metabolic Diseases	Preclinical	GB	University of Glasgow	06 Mar 2020
Metabolic Diseases	Preclinical	DK	University of Southern Denmark	06 Mar 2020
Inflammation	Preclinical	DK	IT-Universitetet I København	-