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Firazorexton | Firazorexton : Agonist of HCRTR2
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (3 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
HCRTR2
  • Kd:85 nM
  • EC50:19 nM
  • EC50:37 nM
  • EC50:170 nM
  • EC50:100 nM
  • EC50:19.7 nM
Agonist
up to 1 uM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
More than 700-fold OX2R selectivity over OX1R (calcium mobilization using hOX1R/CHO-K1 cells was 14, ...
In Cell Selectivity Assessment
Potency Assay Off-Target:
Selectivity vs hOX1R was assessed in CHO-K1 cells showing EC50 14000 nM

Potency
Cellular
In Vitro

HCRTR2

Mode of Action: Agonist

Structure-Activity-Relationship data available? No

DOI Reference: 10.1124/jpet.122.001449

In Vivo Validations

Mouse
Dose: 10 mg/Kg
Route of delivery: Oral
Plasma half life: 1.10 h (MRT)
Cmax: 2221.5 ng/mL
Tmax: 0.5 h
Area Under the Curve:: 2575.0 ng*h/mL

DOI Reference: 10.1124/jpet.122.001449

Dose: 30 mg/Kg
Route of delivery: Oral
Plasma half life: 1.06 h (MRT)
Cmax: 5966.4 ng/mL
Tmax: 0.5 h
Area Under the Curve:: 6867.7 ng*h/mL

DOI Reference: 10.1124/jpet.122.001449

Dose: 3 mg/Kg
Route of delivery: Oral
Plasma half life: 0.94 h (MRT)
Cmax: 967.5 ng/mL
Tmax: 0.5 h
Area Under the Curve:: 1106.0 ng*h/mL

DOI Reference: 10.1124/jpet.122.001449

Chemical Information

Molecular Formula C22H25F3N2O4S
SMILEs CC(C)(O)C(=O)N1CC[C@H](NS(C)(=O)=O)[C@@H]1Cc1cccc(-c2cc(F)cc(F)c2)c1F
InChI InChI=1S/C22H25F3N2O4S/c1-22(2,29)21(28)27-8-7-18(26-32(3,30)31)19(27)11-13-5-4-6-17(20(13)25)14-9-15(23)12-16(24)10-14/h4-6,9-10,12,18-19,26,29H,7-8,11H2,1-3H3/t18-,19-/m0/s1
Molecular weight 470.15 Da
AlogP 0.0
HBond acceptors 6
HBond donors 2
Atoms 57

Vendors

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Expert Reviews

by SERP
(on 27 Aug 2023 )
Cellular Use Rating
In Model Organisms
There are many compounds indexed against this target in ChEMBL https://www.ebi.ac.uk/chembl/g/#browse/activities/filter/target_chembl_id%3ACHEMBL4792%20AND%20standard_type%3A(%22IC50%22) These can...
by SERP
(on 27 Aug 2023 )
Cellular Use Rating
In Model Organisms
...
by SERP+
(on 14 Oct 2025 )
Cellular Use Rating
In Model Organisms
TAK-994 is a potent OX2R full agonist (KD = 85 nM) with good selectivity against OX1R (>700-fold). TAK-994 (10 μM single dose) was tested against a panel of >100 enzymes, receptors, and ion channels; of...
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