DS-1558

DS-1558 : Agonist of FFAR1

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(1 ratings)

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Probe DS-1558 is in the process of SERP review.

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Information

FFAR1

Agonist

In Vitro Validations

No in Vitro Validations

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): No PPARgamma agonistic activity up to 100µM (https://pubs.acs.org/doi/10.1021/ml500391n). No activity for GPR120 and > 100-fold selectivity over 68 other diverse receptors, ion channels and transporters. Inhibition of CYPs: 1A2 - 7%; 2C9 - 21%; 2D6 - 0%; 3A4 - 5%; no hERG inhibition up to 30 µM

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

DS-1558 is a potent agonist of human (EC50 = 3.7 nM) and rat (EC50 = 12 nM) GPR40 as determined in a calcium flux assay in GPR40-transfected CHO cells. DS-1558 shows good selectivity against PPAR gamma and no activity against GPR120. In addition, DS-1558 revealed > 100-fold selectivity over 68 other diverse receptors, ion channels and transporters. GPR40-mediated effects on glucose-stimulated insulin secretion were confirmed in isolated islets from GPR40 KO and wild-type mice. In vivo PK data is available for rat, dog and monkey. In vivo efficacy was demonstrated in a glucose tolerance model in ZDF rats.

(last updated: 15 Aug 2024 )