JNJ-10397049 | CAS#708275-58-5 | OX2 receptor antagonist

MedKoo Cat#: 525303 | Name: JNJ-10397049

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

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.

Chemical Structure

JNJ-10397049

CAS#708275-58-5

Theoretical Analysis

MedKoo Cat#: 525303

Name: JNJ-10397049

CAS#: 708275-58-5

Chemical Formula: C19H20Br2N2O3

Exact Mass: 481.9841

Molecular Weight: 484.19

Elemental Analysis: C, 47.13; H, 4.16; Br, 33.01; N, 5.79; O, 9.91

Price and Availability

Size	Price	Availability	Quantity
5mg	USD 350.00	2 Weeks
10mg	USD 600.00	2 Weeks

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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

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

JNJ-10397049 is a potent and selective orexin 2 receptor (OX2R) antagonist, with a pKi of 8.3.

In vitro activity:

The results of MTT assay showed that the effect of JNJ-10397049 on NPCs proliferation was concentration dependent (Fig. 2). At 1 and 5 µM of JNJ-10397049, cell proliferation significantly increased (F=55.478, P<0.001). Reference: Anat Cell Biol. 2022 Jun 30;55(2):179-189. https://pubmed.ncbi.nlm.nih.gov/35466086/

In vivo activity:

JNJ10397049 showed profound sleep-promoting effects in rats at all doses tested (5, 25 and 50 mg/kg i.p.). More specifically, JNJ10397049 substantially increased REM, NREM and total sleep-time across the whole 5 hour time-window of recording at all doses tested (Figure 6). Reference: PLoS One. 2011 Jan 28;6(1):e16406. https://pubmed.ncbi.nlm.nih.gov/21307957/

	Solvent	mg/mL	mM
Solubility
	DMF	50.0	103.27
	DMF:PBS (pH 7.2) (1:4)	0.2	0.41
	DMSO	100.0	206.53
	Ethanol	30.0	61.96

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 484.19 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

Formulation protocol:

1. Karami N, Azari H, Rahimi M, Aligholi H, Kalantari T. A study on the effect of JNJ-10397049 on proliferation and differentiation of neural precursor cells. Anat Cell Biol. 2022 Jun 30;55(2):179-189. doi: 10.5115/acb.21.202. Epub 2022 Apr 25. PMID: 35466086; PMCID: PMC9256489. 2. 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. PMID: 21307957; PMCID: PMC3030585. 3. 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. PMID: 19363060.

In vitro protocol:

In vivo protocol:

1. 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. PMID: 21307957; PMCID: PMC3030585. 2. 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. PMID: 19363060.

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. ^