JNJ-10397049
featured

    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.


Price and Availability

Size
Price

5mg
USD 270
Size
Price

10mg
USD 430
Size
Price

JNJ-10397049, 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

img

Theoretical Analysis

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


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).

Harmonized System Code:
293490


References

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. ^