1. GPCR/G Protein Neuronal Signaling
  2. Orexin Receptor (OX Receptor)
  3. Ledasorexton

Ledasorexton is an orally active OX2R agonist (EC50: 0.99 nM). Ledasorexton has awakening effect in mice. Ledasorexton can be used for research of neurological disease.

For research use only. We do not sell to patients.

Ledasorexton

Ledasorexton Chemical Structure

CAS No. : 2758363-88-9

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Description

Ledasorexton is an orally active OX2R agonist (EC50: 0.99 nM). Ledasorexton has awakening effect in mice. Ledasorexton can be used for research of neurological disease[1].

IC50 & Target[1]

OX2 Receptor

0.99 nM (EC50)

OX1 Receptor

>100 nM (EC50)

In Vitro

Ledasorexton (Example 1) exhibits potent agonist activity against hOX2R with an EC50 of 0.99 nM, while showing weak activity against hOX1R (EC50 > 100 nM) in HEK293 cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Ledasorexton (Example 1) (0.3, 1, 3 or 10 mg/kg, i.g., single dose) shows awakening effect in mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Orexin/ataxin-3 Tg mice (10-14 weeks old)[1]
Dosage: 0.3, 1, and 3 mg/kg
Administration: i.g., single dose
Result: Significantly prolonged sleep latency at 1 and 3 mg/kg.
Significantly suppressed cataplexy-like symptoms at 3 mg/kg.
Animal Model: Male wild-type (WT) C57BL/6 mice (13 weeks old)[1]
Dosage: 1, 3 and 10 mg/kg
Administration: i.g., single dose
Result: Significantly increased spontaneous activity in mice.
Significantly increased sleep latency at 3 or 10 mg/kg.
Molecular Weight

417.52

Formula

C22H32FN5O2

CAS No.
SMILES

NC([C@@H](C1CC1)N2[C@@]3([H])C[C@]([C@]4([H])[C@@H](CN(C5=NC=C(F)C=N5)CC4)OC)([H])C[C@]2([H])CC3)=O

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
Ledasorexton
Cat. No.:
HY-177096
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