DANAVOREXTON | DANAVOREXTON : Agonist of HCRTR2
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (3 reviews)
Control Compounds

Probe Summary

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Targets Biochemical/Biophysical Potency Cellular Potency
HCRTR2
  • Kd:48 nM
  • EC50:5.5 nM
  • EC50:15 nM
Agonist
300 nM - 1µM
100 nM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
Within target family - T-516 (TAK-925 analog) had a > 6000-fold OX2R selectivity against OX1R in cal ...

Potency
Cellular
In Vitro

HCRTR2

Mode of Action: Agonist

Structure-Activity-Relationship data available? No

DOI Reference: 10.1016/j.pbb.2019.172794

In Vivo Validations

Mouse
Dose: 3 mg/Kg
Route of delivery: Subcutaneous
Organ of interest (O): Brain

DOI Reference: 10.1016/j.pbb.2019.172794

Orthogonal Probes def

CANSAR1744939

Chemical Information

Molecular Formula C21H32N2O5S
SMILEs COC(=O)N1CCC[C@H](NS(C)(=O)=O)[C@@H]1CO[C@H]1CC[C@@H](c2ccccc2)CC1
InChI InChI=1S/C21H32N2O5S/c1-27-21(24)23-14-6-9-19(22-29(2,25)26)20(23)15-28-18-12-10-17(11-13-18)16-7-4-3-5-8-16/h3-5,7-8,17-20,22H,6,9-15H2,1-2H3/t17-,18+,19-,20-/m0/s1
Molecular weight 424.20 Da
AlogP 2.878000000000001
HBond acceptors 7
HBond donors 1
Atoms 61

Vendors

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Expert Reviews


(on 19 Apr 2022)
Cellular Use Rating
In Model Organisms
Sufficient brain concentrations are achieved in the mouse, however, the authors note that a short plasma half-life is observed.
(on 8 Jul 2022)
In Model Organisms
(The reviewer did not leave any public comments)
(on 14 Oct 2025)
Cellular Use Rating
In Model Organisms
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...
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