SB649868
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MedKoo CAT#: 526934

CAS#: 380899-24-1

Description: SB649868, also known as GSK-649868, is an orexin receptor antagonist potentially for the treatment of insomnia and sleep disorder. SB-649868 promotes and maintains sleep in men with primary insomnia. SB-649868 may be a potentially effective and well-tolerated treatments for patients with sleep disorders.


Price and Availability

Size Price Shipping out time Quantity
100mg USD 1550 2 Weeks
200mg USD 2150 2 Weeks
500mg USD 2950 2 Weeks
1g USD 3850 2 Weeks
2g USD 5250 2 Weeks
Inquire bulk and customized quantity

Pricing updated 2020-10-23. Prices are subject to change without notice.

SB649868, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 526934
Name: SB649868
CAS#: 380899-24-1
Chemical Formula: C26H24FN3O3S
Exact Mass: 477.1522
Molecular Weight: 477.5544
Elemental Analysis: C, 65.39; H, 5.07; F, 3.98; N, 8.80; O, 10.05; S, 6.71


Synonym: GSK-649868; GSK-649868; GSK649868; SB649868; SB-649868; SB 649868.

IUPAC/Chemical Name: (S)-N-((1-(5-(4-fluorophenyl)-2-methylthiazole-4-carbonyl)piperidin-2-yl)methyl)benzofuran-4-carboxamide

InChi Key: ZJXIUGNEAIHSBI-IBGZPJMESA-N

InChi Code: InChI=1S/C26H24FN3O3S/c1-16-29-23(24(34-16)17-8-10-18(27)11-9-17)26(32)30-13-3-2-5-19(30)15-28-25(31)21-6-4-7-22-20(21)12-14-33-22/h4,6-12,14,19H,2-3,5,13,15H2,1H3,(H,28,31)/t19-/m0/s1

SMILES Code: O=C(C1=C2C=COC2=CC=C1)NC[C@H]3N(C(C4=C(C5=CC=C(F)C=C5)SC(C)=N4)=O)CCCC3


Technical Data

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code:
2934.99.9001


References

1: Jacobson LH, Callander GE, Hoyer D. Suvorexant for the treatment of insomnia. Expert Rev Clin Pharmacol. 2014 Nov;7(6):711-30. doi: 10.1586/17512433.2014.966813. Review. PubMed PMID: 25318834.

2: Patel AX, Miller SR, Nathan PJ, Kanakaraj P, Napolitano A, Lawrence P, Koch A, Bullmore ET. Neuroendocrine and sympathetic responses to an orexin receptor antagonist, SB-649868, and alprazolam following insulin-induced hypoglycemia in humans. Psychopharmacology (Berl). 2014 Oct;231(19):3817-28. doi: 10.1007/s00213-014-3520-7. PubMed PMID: 24770625; PubMed Central PMCID: PMC4159598.

3: Hoyer D, Jacobson LH. Orexin in sleep, addiction and more: is the perfect insomnia drug at hand? Neuropeptides. 2013 Dec;47(6):477-88. doi: 10.1016/j.npep.2013.10.009. Review. PubMed PMID: 24215799.

4: Pałasz A, Lapray D, Peyron C, Rojczyk-Gołębiewska E, Skowronek R, Markowski G, Czajkowska B, Krzystanek M, Wiaderkiewicz R. Dual orexin receptor antagonists - promising agents in the treatment of sleep disorders. Int J Neuropsychopharmacol. 2014 Jan;17(1):157-68. doi: 10.1017/S1461145713000552. Review. Erratum in: Int J Neuropsychopharmacol. 2016;19(3). pii: pyw005. doi: 10.1093/ijnp/pyw005. PubMed PMID: 23702225.

5: Bettica P, Squassante L, Zamuner S, Nucci G, Danker-Hopfe H, Ratti E. The orexin antagonist SB-649868 promotes and maintains sleep in men with primary insomnia. Sleep. 2012 Aug 1;35(8):1097-104. doi: 10.5665/sleep.1996. PubMed PMID: 22851805; PubMed Central PMCID: PMC3397789.

6: Faedo S, Perdonà E, Antolini M, di Fabio R, Merlo Pich E, Corsi M. Functional and binding kinetic studies make a distinction between OX1 and OX2 orexin receptor antagonists. Eur J Pharmacol. 2012 Oct 5;692(1-3):1-9. doi: 10.1016/j.ejphar.2012.07.007. PubMed PMID: 22796453.

7: Bettica P, Squassante L, Groeger JA, Gennery B, Winsky-Sommerer R, Dijk DJ. Differential effects of a dual orexin receptor antagonist (SB-649868) and zolpidem on sleep initiation and consolidation, SWS, REM sleep, and EEG power spectra in a model of situational insomnia. Neuropsychopharmacology. 2012 Apr;37(5):1224-33. doi: 10.1038/npp.2011.310. PubMed PMID: 22237311; PubMed Central PMCID: PMC3306884.

8: Bettica P, Nucci G, Pyke C, Squassante L, Zamuner S, Ratti E, Gomeni R, Alexander R. Phase I studies on the safety, tolerability, pharmacokinetics and pharmacodynamics of SB-649868, a novel dual orexin receptor antagonist. J Psychopharmacol. 2012 Aug;26(8):1058-70. doi: 10.1177/0269881111408954. PubMed PMID: 21730017.

9: Renzulli C, Nash M, Wright M, Thomas S, Zamuner S, Pellegatti M, Bettica P, Boyle G. Disposition and metabolism of [14C]SB-649868, an orexin 1 and 2 receptor antagonist, in humans. Drug Metab Dispos. 2011 Feb;39(2):215-27. doi: 10.1124/dmd.110.035386. Erratum in: Drug Metab Dispos. 2011 Jun;39(6):1111. PubMed PMID: 21045199.