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SB-649868

Chemical Structure : SB-649868

CAS No.: 380899-24-1

SB-649868 (SB 649868;SB649868)

Catalog No.: PC-60755Not For Human Use, Lab Use Only.

A potent, selective, orally bioavailable, dual orexin OX1/OX2R antagonist with pKi of 9.4 and 9.5 respectively.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

A potent, selective, orally bioavailable, dual orexin OX1/OX2R antagonist with pKi of 9.4 and 9.5 respectively; displays >1,000-fold selectivity for the orexin target receptors in a broad panel of GPCRs, ion channels and enzymes; demonstrates high effectivity in pre-clinical model of sleep disorders.

Sleep Disorder

Phase 2 Discontinued

Physicochemical Properties

M.Wt 477.554
Formula C26H24FN3O3S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(S)-N-((1-(5-(4-fluorophenyl)-2-methylthiazole-4-carbonyl)piperidin-2-yl)methyl)benzofuran-4-carboxamide

References

1. Renzulli C, et al. Drug Metab Dispos. 2011 Feb;39(2):215-27.

2. Bettica P, et al .Neuropsychopharmacology. 2012 Apr;37(5):1224-33.

3. Piccoli L, et al. Neuropsychopharmacology. 2012 Aug;37(9):1999-2011.

4. Di Fabio R, et al. Bioorg Med Chem Lett. 2011 Sep 15;21(18):5562-7.

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