TENAPANOR

TENAPANOR : Inhibitor of SLC9A3

Structure

SERP Rating

In Cells

(0 ratings)

In Model Organisms

(1 ratings)

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Probe TENAPANOR is in the process of SERP review.

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Information

SLC9A3

Inhibitor

100 nM
Reviewer recommended concentration: 0.1-10 mg/kg in rats.. Statistically significant effects can be seen at 0.1 mg/kg in some cases. The authors also note "dehydration was observed due to the exaggerated PD response (i.e., diarrhea) at the studied dose (30 mg/kg).

Probe Availability:

In Vitro Validations

No in Vitro Validations

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

The potency of Tenapanor was tested against NHE1, NHE2, NHE3, NaPiIIb, TGR5, ASBT, and Pit-1. Excluding NHE3, all targets showed IC50 >10uM

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SERP ratings and comments

SERP Ratings

In Model Organisms

SERP Comments:

Tenapanor is an approved drug targeting the Intestinal Na+/H+ Exchanger Isoform 3 (SLC9A3/NHE3). It has excellent selectivity versus other intestinal transporters and is well tolerated. Rats appear to have higher sensitivity to Tenapanor than humans. The drug has very low oral bioavailability in rats, dogs, and humans so has minimal systemic exposure in line with its good safety profile.

(last updated: 27 Jun 2022 )