JNJ 10397049

  • CAT Number: R015878
  • CAS Number: 708275-58-5
  • Molecular Formula: C19H20Br2N2O3
  • Molecular Weight: 484.188
  • Purity: ≥95%
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JNJ 10397049 (Cat. No: R015878) is an efficient and selective inhibitor of the orexin 2 receptor. Its activity to the OX2 receptor is much higher than that to the OX1 receptor. This product is mainly used for preclinical and scientific research.

Catalog Number R015878
CAS Number 708275-58-5
Molecular Formula

C19H20Br2N2O3

Purity 95%
Target OX Receptor
Solubility Soluble in DMSO > 10 mM
Storage Store at +4C
IUPAC Name 1-(2,4-dibromophenyl)-3-[(4S,5S)-2,2-dimethyl-4-phenyl-1,3-dioxan-5-yl]urea
InChI InChI=1S/C19H20Br2N2O3/c1-19(2)25-11-16(17(26-19)12-6-4-3-5-7-12)23-18(24)22-15-9-8-13(20)10-14(15)21/h3-10,16-17H,11H2,1-2H3,(H2,22,23,24)/t16-,17-/m0/s1
InChIKey RBKIJGLHFFQHBE-IRXDYDNUSA-N
SMILES CC1(OCC(C(O1)C2=CC=CC=C2)NC(=O)NC3=C(C=C(C=C3)Br)Br)C
Reference

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1: Mavanji V, Perez-Leighton CE, Kotz CM, Billington CJ, Parthasarathy S, Sinton CM, Teske JA. Promotion of Wakefulness and Energy Expenditure by Orexin-A in the Ventrolateral Preoptic Area. Sleep. 2015 Sep 1;38(9):1361-70. doi: 10.5665/sleep.4970. PubMed PMID: 25845696; PubMed Central PMCID: PMC4531404.<br />
2: Dugovic C, Shelton JE, Yun S, Bonaventure P, Shireman BT, Lovenberg TW. Orexin-1 receptor blockade dysregulates REM sleep in the presence of orexin-2 receptor antagonism. Front Neurosci. 2014 Feb 14;8:28. doi: 10.3389/fnins.2014.00028. eCollection 2014. PubMed PMID: 24592208; PubMed Central PMCID: PMC3924048.<br />
3: Cataldi NI, Lux Lantos VA, Libertun C. Orexin A and B in vitro modify orexins receptors expression and gonadotropins secretion of anterior pituitary cells of proestrous rats. Regul Pept. 2014 Jan 10;188:25-30. doi: 10.1016/j.regpep.2013.12.002. Epub 2013 Dec 12. PubMed PMID: 24333629.<br />
4: Faedo S, Perdon&agrave; 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. Epub 2012 Jul 13. PubMed PMID: 22796453.<br />
5: Cataldi NI, Lux-Lantos VA, Libertun C. Effects of orexins A and B on expression of orexin receptors and progesterone release in luteal and granulosa ovarian cells. Regul Pept. 2012 Oct 10;178(1-3):56-63. doi: 10.1016/j.regpep.2012.06.008. Epub 2012 Jun 29. PubMed PMID: 22749989.<br />
6: Piccoli L, Micioni Di Bonaventura MV, Cifani C, Costantini VJ, Massagrande M, Montanari D, Martinelli P, Antolini M, Ciccocioppo R, Massi M, Merlo-Pich E, Di Fabio R, Corsi M. Role of orexin-1 receptor mechanisms on compulsive food consumption in a model of binge eating in female rats. Neuropsychopharmacology. 2012 Aug;37(9):1999-2011. doi: 10.1038/npp.2012.48. Epub 2012 May 9. PubMed PMID: 22569505; PubMed Central PMCID: PMC3398727.<br />
7: Gozzi A, Turrini G, Piccoli L, Massagrande M, Amantini D, Antolini M, Martinelli P, Cesari N, Montanari D, Tessari M, Corsi M, Bifone A. Functional magnetic resonance imaging reveals different neural substrates for the effects of orexin-1 and orexin-2 receptor antagonists. PLoS One. 2011 Jan 28;6(1):e16406. doi: 10.1371/journal.pone.0016406. PubMed PMID: 21307957; PubMed Central PMCID: PMC3030585.<br />
8: Shoblock JR, Welty N, Aluisio L, Fraser I, Motley ST, Morton K, Palmer J, Bonaventure P, Carruthers NI, Lovenberg TW, Boggs J, Galici R. Selective blockade of the orexin-2 receptor attenuates ethanol self-administration, place preference, and reinstatement. Psychopharmacology (Berl). 2011 May;215(1):191-203. doi: 10.1007/s00213-010-2127-x. Epub 2010 Dec 22. PubMed PMID: 21181123.<br />
9: Dugovic C, Shelton JE, Aluisio LE, Fraser IC, Jiang X, Sutton SW, Bonaventure P, Yun S, Li X, Lord B, Dvorak CA, Carruthers NI, Lovenberg TW. Blockade of orexin-1 receptors attenuates orexin-2 receptor antagonism-induced sleep promotion in the rat. J Pharmacol Exp Ther. 2009 Jul;330(1):142-51. doi: 10.1124/jpet.109.152009. Epub 2009 Apr 10. PubMed PMID: 19363060.<br />
10: Silveyra P, Lux-Lantos V, Libertun C. Both orexin receptors are expressed in rat ovaries and fluctuate with the estrous cycle: effects of orexin receptor antagonists on gonadotropins and ovulation. Am J Physiol Endocrinol Metab. 2007 Oct;293(4):E977-85. Epub 2007 Jul 17. PubMed PMID: 17638707. ^<br />
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