WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 525303
CAS#: 708275-58-5
Description: JNJ-10397049 is a potent and selective OX2 receptor antagonist (pIC50 = 7.4 for chimeric OX2 receptors; pKB values are 5.9 and 8.5 for OX1 and OX2 receptors respectively). It shows no significant activity in a panel of over 50 other neurotransmitters and neuropeptide receptors. JNJ-10397049 achieves high level of OX2 receptor occupancy in the rat brain.
MedKoo Cat#: 525303
Name: JNJ-10397049
CAS#: 708275-58-5
Chemical Formula: C19H20Br2N2O3
Exact Mass: 481.98407
Molecular Weight: 484.18
Elemental Analysis: C, 47.13; H, 4.16; Br, 33.01; N, 5.79; O, 9.91
Synonym: JNJ-10397049; JNJ 10397049; JNJ10397049.
IUPAC/Chemical Name: 1-(2,4-Dibromophenyl)-3-((4S,5S)-2,2-dimethyl-4-phenyl-(1,3)dioxan-5-yl)urea
InChi Key: RBKIJGLHFFQHBE-IRXDYDNUSA-N
InChi Code: 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
SMILES Code: CC1(OC[C@@H]([C@@H](O1)c2ccccc2)NC(=O)Nc3ccc(cc3Br)Br)C
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
The following data is based on the product molecular weight 484.18 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
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.
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.
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.
4: 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. Epub 2012 Jul 13. PubMed PMID: 22796453.
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.
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.
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.
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.
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.
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. ^
