GW1100

GW1100 : Antagonist of FFAR1

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(1 ratings)

note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars.

Probe GW1100 is in the process of SERP review.

Please continue to check back for new reviews and commentary.

Information

FFAR1

Antagonist

up to 10 uM

Probe Availability:

In Vitro Validations

No in Vitro Validations

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Cell:

GW1100 has no effect on the GPR120‐mediated stimulation of intracellular Ca2+ release; is shown to be selective against 220 other GPCRs Outside target family: At least 100‐fold selective against 60 kinases, 63 proteases, seven integrins and 20 nuclear receptors including PPARα, δ and γ, with the exception of the oxytocin receptor, for which it acted as an antagonist with a pIC50 6.9

I have extra information to add

SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

GW1100 is a standard cellular and in vivo tool for antagonizing FFAR1/GPR120. It is commonly used to counteract the affects of GPR120 agonist GW9508 and long chain fatty acids. However, the in vivo mouse work in the referenced paper does not consider body weight of the mouse, only that 10ug of material was injected. In one rat study, GW1100 was applied intranasally, although the methods section does not detail the dose. https://doi.org/10.1186/s12974-021-02209-9

(last updated: 1 Dec 2021 )