ERTUGLIFLOZIN

ERTUGLIFLOZIN : Inhibitor of SLC5A2

Structure

SERP Rating

In Cells

(2 ratings)

In Model Organisms

(2 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 ERTUGLIFLOZIN is in the process of SERP review.

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Information

SLC5A2

Inhibitor

up to 100 nM

Probe Availability:

In Vitro Validations

No in Vitro Validations

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): Selectivity within target family: Selective against h-SGLT1 IC50 2050 (>2000 fold)

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

As a selective inhibitor, ERTUGLIFLOZIN exhibits excellent potency and selectivity in vitro, and good pharmacokinetics in vivo. However, it should be noted that information regarding off-target is still insufficient. Nevertheless, based on its outstanding performance and low side effects as a marketed drug (N Engl J Med. 2020, 383(15):1425-1435; Medicine (Baltimore). 2023, 102(10):e33198.), it can be inferred that it's risk of interactions with other functional proteins is low. Furthermore, compared to other drugs of the same class (Dapagliflozin, Canagliflozin, Empagliflozin, Ipragliflozin, Tofogliflozin), it can be considered as one of the best in that category (Eur J Med Chem. 2019, 184:111773). Therefore, it is strongly recommended as a tool probe for cellular and in vivo studies.

(last updated: 7 Nov 2023 )

SERP Ratings

In Cell Rating

In Model Organisms

(last updated: 30 Dec 2023 )