Firazorexton

Firazorexton : Agonist of HCRTR2

Structure

SERP Rating

In Cells

(2 ratings)

In Model Organisms

(2 ratings)

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Probe Firazorexton is in the process of SERP review.

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Information

HCRTR2

Agonist

up to 1 uM

Probe Availability:

MedChemExpress

In Vitro Validations

Uniprot ID: O43614

Target Class: GPCR

Target SubClass: Orexin receptor

Potency: Kd

Potency Value: 85 nM

Potency Assay: Radioligand Binding Assay (Saturation Binding assay), Bmax of 4.03 pmol/mg protein

PDB ID for probe-target interaction (3D structure): --

Target aliases:

Orexin receptor type 2, HCRTR2, OX2R_HUMAN, Ox2R, ...

DOI Reference: 10.1124/jpet.122.001449

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): More than 700-fold OX2R selectivity over OX1R (calcium mobilization using hOX1R/CHO-K1 cells was 14,000 nM). The inhibitory or stimulatory activities of TAK-994 against various enzymes, receptors, and ion channels (106 targets in total) were assessed. TAK-994 at 10 μM did not induce more than 50% inhibition or stimulation of any enzymes, receptors, and ion channels, except progesterone receptor B (55% inhibition), indicating high selectivity of TAK-994 for OX2R with minimal off-target activity in vitro

Potency assay, off target (cells): Selectivity vs hOX1R was assessed in CHO-K1 cells showing EC50 14000 nM

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

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 be inspected for low-activity contro compounds and orthogonal probes. The PubChem entry for this compound is https://pubchem.ncbi.nlm.nih.gov/compound/137460733

(last updated: 27 Aug 2023 )

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

An exceptionally well characterized probe compound, with demonstrated in vivo (po in mouse) and in cell pharmacology and pharmacodynamic activity. Orally bioavailable, cell-permeable and brain penetrant.

(last updated: 27 Aug 2023 )