DANAVOREXTON

DANAVOREXTON : Agonist of HCRTR2

Structure

SERP Rating

In Cells

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In Model Organisms

(2 ratings)

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Information

HCRTR2

Agonist

100 nM

Probe Availability:

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 )