GSK1016790A

GSK1016790A : Agonist of TRPV4

Structure

Information

  • TRPV4
  • Agonist
  • 10 nM
  • Reviewer recommended concentration: 100 nM and below

In Vitro Validations

No in Vitro Validations

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): No activity is detectable versus the highly homologous TRP vanilloid subtype 1 (V1) cation channel, as assessed by Ca2+ influx studies in TRPV1-transduced cells.
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SERP ratings and comments


SERP Ratings

In Cell Rating

SERP Comments:

This probe is a highly potent agonist of TRPV4. The available data use complementary cell based assays to establish that human TRPV4 is activated with EC50 3-5 nM while mouse TRPV4 potency is somewhat lower, 18 nM. This species difference may influence choice of concentration for use in cell-based studies. This probe also potently activates TRPV4 in mouse bladder tissue (100 nM used in those studies). While this probe is a strong choice for experiments using cell and tissues and lacks affinity for TRPV1, no broader profiling of GPCRs is available and potent off-target effects are possible. The reported lethal on-target effects in vivo preclude therapeutic use in animal models.

(last updated: 27 Nov 2023 )

SERP Ratings

In Cell Rating

(last updated: 7 Dec 2023 )