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SB-649868

SB-649868 is a potent and selective orally active orexin (OX) 1 and OX2 receptor antagonist (pKi =9.4 and 9.5 at the OX1 and OX2 receptor, respectively) .

Product Specifications

CAS Number

[380899-24-1]

Product Name Alternative

GSK649868

UNSPSC

12352005

Hazard Statement

H315, H319, H335

Target

Orexin Receptor (OX Receptor)

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Metabolism-protein/nucleotide metabolism

Field of Research

Metabolic Disease; Endocrinology

Assay Protocol

https://www.medchemexpress.com/SB-649868.html

Purity

99.87

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C(C1=C(C2=CC=C(F)C=C2)SC(C)=N1)N3CCCC[C@H]3CNC(C4=C(C=CO5)C5=CC=C4)=O

Molecular Formula

C26H24FN3O3S

Molecular Weight

477.55

Precautions

H315, H319, H335

References & Citations

[1]Di Fabio R, et al. Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2receptor antagonist useful for treatment of sleep disorders. Bioorg Med Chem Lett. 2011 Sep 15;21 (18) :5562-7.|[2]Faedo S, et al. Functional and binding kinetic studies make a distinction between OX1 and OX2 orexin receptorantagonists. Eur J Pharmacol. 2012 Oct 5;692 (1-3) :1-9.

Shipping Conditions

Room Temperature

Storage Conditions

-20°C, 3 years; 4°C, 2 years (Powder)

Scientific Category

Reference compound1

Clinical Information

Phase 2

Isoform

OX2 Receptor

Available Sizes

Curated Selection

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