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DANAVOREXTON

DANAVOREXTON : Agonist of HCRTR2

Structure

Information

  • HCRTR2
  • Agonist
  • 100 nM
  • Reviewer recommended concentration: 300 nM - 1µM

In Vitro Validations

Uniprot ID: O43614
Target Class: GPCR
Target SubClass: Orexin 2 receptor
Potency: Kd
Potency Value: 48 nM
Potency Assay: Binding assay using [3H]T-516 (TAK-925 Analog) bound to the membrane fractions of hOX2R-transfected Expi293F cells with a single saturable high-affinity binding site.
PDB ID for probe-target interaction (3D structure): --
Target aliases:
Orexin receptor type 2, HCRTR2, OX2R_HUMAN, Ox2R, ...

DOI Reference: 10.1016/j.pbb.2019.172794

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:
Within target family - T-516 (TAK-925 analog) had a > 6000-fold OX2R selectivity against OX1R in calcium mobilization assays (EC50: 4.3 nM for OX2R and > 30,000 nM for OX1R). Outside target family - Selectivity of TAK-925 was characterized by measuring its inhibitory or stimulatory activities against enzymes and receptors. >50% inhibition or stimulation by 10 μM of TAK-925 was considered to be a significant response. TAK-925 did not induce a significant response in 106 target molecules.
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SERP ratings and comments

SERP Ratings

In Cell Rating
In Model Organisms

SERP Comments:

Sufficient brain concentrations are achieved in the mouse, however, the authors note that a short plasma half-life is observed.

(last updated: 19 Apr 2022 )

SERP Ratings

In Model Organisms

(last updated: 8 Jul 2022 )

SERP+ Ratings

In Cell Rating
In Model Organisms

SERP+ Comments:

This is a highly potent and selective full agonist of human OX2R, with a range of functional characterisation. However, no cytotoxicity data reported, so the upper limit for suitable concentration is not defined. Functional changes (biomarkers) are evaluated in mouse, although binding and activity not measured for mouse receptor.

(last updated: 14 Oct 2025 )