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SL-88. Free Fatty Acid Receptor Regulators The nonesterified or “free” fatty acids (FFA) family of receptors are receiving interest as novel targets for the treatment of metabolic and inflammatory diseases [1]. Understanding of the complex pharmacology of these receptors using small molecule probing tools is critical for unlocking their rich therapeutic potential. For many members of this receptor family both agonist and antagonsits modulators have been reported [1]. Known small molecule agonists of FFA receptors share some common pharmacophoric features, such as a carboxylic acid moiety attached directly or via an aliphatic tail to an aromatic core. A pharmacophore search through ASINEX’s compound collection identified several hits that can be explored for FFA research and drug discovery. Signature Library 88 Formats Supplementary Information 80 compounds per plate 0.1 mg; 1 mg; 2 mg dry film/powder 0.1 µmol; 1 µmol DMSO solutions SL#88_FFAR_reg.sdf References: 1. Chem. Rev., 2017, 117 (1), pp 67–110. doi: 10.1021/acs.chemrev.6b00056 Contact us: USA: +1 336 721 1617 [email protected] Japan: +81-80-3401-9097 [email protected] Europe/Global: [email protected] LAS 51190849 LAS 51202179 O O O HO CH 3 CH 3 H 3 C H H LAS 51190167 GW9508 (FFA1 agoinist) Cmpd 44 (FFA2 agonist) Cmpd 60 (FFA4 agoinist)

SL-88 FFAR Regulators · 2019. 11. 25. · Title: Microsoft Word - SL-88_FFAR Regulators Author: shing Created Date: 11/12/2018 8:37:16 PM

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Page 1: SL-88 FFAR Regulators · 2019. 11. 25. · Title: Microsoft Word - SL-88_FFAR Regulators Author: shing Created Date: 11/12/2018 8:37:16 PM

SL-88. Free Fatty Acid Receptor Regulators

The nonesterified or “free” fatty acids (FFA) family of receptors are receiving interest as novel targets for the treatment of metabolic and inflammatory diseases [1]. Understanding of the complex pharmacology of these receptors using small molecule probing tools is critical for unlocking their rich therapeutic potential. For many members of this receptor family both agonist and antagonsits modulators have been reported [1].

Known small molecule agonists of FFA receptors share some common pharmacophoric features, such as a carboxylic acid moiety attached directly or via an aliphatic tail to an aromatic core. A pharmacophore search through ASINEX’s compound collection identified several hits that can be explored for FFA research and drug discovery.

Signature Library 88 Formats Supplementary Information 80 compounds per plate 0.1 mg; 1 mg; 2 mg dry film/powder 0.1 µmol; 1 µmol DMSO solutions

SL#88_FFAR_reg.sdf

References:

1. Chem. Rev., 2017, 117 (1), pp 67–110. doi: 10.1021/acs.chemrev.6b00056

Contact us: USA: +1 336 721 1617 [email protected] Japan: +81-80-3401-9097 [email protected] Europe/Global: [email protected]

LAS 51190849

LAS 51202179

O

OOHO

CH3

CH3H3C

H

H

LAS 51190167

GW9508 (FFA1 agoinist)

Cmpd 44 (FFA2 agonist)

Cmpd 60 (FFA4 agoinist)

Page 2: SL-88 FFAR Regulators · 2019. 11. 25. · Title: Microsoft Word - SL-88_FFAR Regulators Author: shing Created Date: 11/12/2018 8:37:16 PM