JNJ7777120 | CAS#459168-41-3 | H4 receptor antagonist

MedKoo Cat#: 522409 | Name: JNJ7777120

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Description:

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

JNJ7777120 is a potent and selective histamine H4 receptor antagonist. JNJ7777120 induces increases in the histamine content of the rat conjunctiva. In vivo studies showed that JNJ7777120 significantly suppressed nasal symptoms and the number of coughs. JNJ7777120 significantly inhibited airway reactivity to histamine.

Chemical Structure

JNJ7777120

CAS#459168-41-3

Theoretical Analysis

MedKoo Cat#: 522409

Name: JNJ7777120

CAS#: 459168-41-3

Chemical Formula: C14H16ClN3O

Exact Mass: 277.0982

Molecular Weight: 277.75

Elemental Analysis: C, 60.54; H, 5.81; Cl, 12.76; N, 15.13; O, 5.76

Price and Availability

Size	Price	Availability
5mg	USD 280.00
10mg	USD 450.00	2 Weeks
25mg	USD 850.00	2 Weeks

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Synonym

JNJ7777120; JNJ-7777120; JNJ 7777120.

IUPAC/Chemical Name

1-[(5-Chloro-1H-indol-2-yl)carbonyl]-4-methylpiperazine

InChi Key

HUQJRYMLJBBEDO-UHFFFAOYSA-N

InChi Code

InChI=1S/C14H16ClN3O/c1-17-4-6-18(7-5-17)14(19)13-9-10-8-11(15)2-3-12(10)16-13/h2-3,8-9,16H,4-7H2,1H3

SMILES Code

CN1CCN(C(C(N2)=CC3=C2C=CC(Cl)=C3)=O)CC1

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, not in water

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-7777120 is a selective H4R antagonist with Ki of 4 ±1 nM, exhibits >1000-fold selectivity over the other histamin receptors.

In vitro activity:

JNJ 7777120 blocks histamine-induced chemotaxis and calcium influx in mouse bone marrow-derived mast cells. Reference: J Pharmacol Exp Ther. 2004 Apr;309(1):404-13. https://pubmed.ncbi.nlm.nih.gov/14722321/

In vivo activity:

The treatment with JNJa (JNJ7777120 20 mg/kg) (1809 cm) and JNJb (JNJ7777120 40 mg/kg) (2111 cm) increased the locomotor activity of mild stress rats, the effect being similar to those produced by the known antidepressant drugs. In the case of JNJ the effect was dose-dependent, the locomotor activity in group JNJb being significantly increased compared with the one obtained for the group JNJa. Reference: J Pers Med. 2022 Feb 9;12(2):246. https://pubmed.ncbi.nlm.nih.gov/35207733/

	Solvent	mg/mL	mM
Solubility
	DMF:PBS (pH 7.2) (1:1)	0.5	1.80
	DMSO	33.5	120.51
	Ethanol	5.0	18.00

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 277.75 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. Thurmond RL, Desai PJ, Dunford PJ, Fung-Leung WP, Hofstra CL, Jiang W, Nguyen S, Riley JP, Sun S, Williams KN, Edwards JP, Karlsson L. A potent and selective histamine H4 receptor antagonist with anti-inflammatory properties. J Pharmacol Exp Ther. 2004 Apr;309(1):404-13. doi: 10.1124/jpet.103.061754. Epub 2004 Jan 13. PMID: 14722321. 2. Yeni Y, Cakir Z, Hacimuftuoglu A, Taghizadehghalehjoughi A, Okkay U, Genc S, Yildirim S, Saglam YS, Calina D, Tsatsakis A, Docea AO. A Selective Histamine H4 Receptor Antagonist, JNJ7777120, Role on glutamate Transporter Activity in Chronic Depression. J Pers Med. 2022 Feb 9;12(2):246. doi: 10.3390/jpm12020246. PMID: 35207733; PMCID: PMC8880293. 3. Dettori I, Gaviano L, Melani A, Lucarini L, Durante M, Masini E, Pedata F. A Selective Histamine H4 Receptor Antagonist, JNJ7777120, Is Protective in a Rat Model of Transient Cerebral Ischemia. Front Pharmacol. 2018 Oct 29;9:1231. doi: 10.3389/fphar.2018.01231. PMID: 30420807; PMCID: PMC6215858.

In vitro protocol:

In vivo protocol:

1. Yeni Y, Cakir Z, Hacimuftuoglu A, Taghizadehghalehjoughi A, Okkay U, Genc S, Yildirim S, Saglam YS, Calina D, Tsatsakis A, Docea AO. A Selective Histamine H4 Receptor Antagonist, JNJ7777120, Role on glutamate Transporter Activity in Chronic Depression. J Pers Med. 2022 Feb 9;12(2):246. doi: 10.3390/jpm12020246. PMID: 35207733; PMCID: PMC8880293. 2. Dettori I, Gaviano L, Melani A, Lucarini L, Durante M, Masini E, Pedata F. A Selective Histamine H4 Receptor Antagonist, JNJ7777120, Is Protective in a Rat Model of Transient Cerebral Ischemia. Front Pharmacol. 2018 Oct 29;9:1231. doi: 10.3389/fphar.2018.01231. PMID: 30420807; PMCID: PMC6215858.

1: Kovacova-Hanuskova E, Gavliakova S, Buday T, Kosutova P, Mokra D, Urbanova-Fulmekova A, Mokry J, Plevkova J. The effect of selective antagonist of H4 receptor JNJ7777120 on nasal symptoms, cough, airway reactivity and inflammation in guinea pigs. Respir Physiol Neurobiol. 2015 Sep 15;216:9-14. doi: 10.1016/j.resp.2015.05.007. Epub 2015 May 21. PubMed PMID: 26003849. 2: Rosa AC, Pini A, Lucarini L, Lanzi C, Veglia E, Thurmond RL, Stark H, Masini E. Prevention of bleomycin-induced lung inflammation and fibrosis in mice by naproxen and JNJ7777120 treatment. J Pharmacol Exp Ther. 2014 Nov;351(2):308-16. doi: 10.1124/jpet.114.215152. Epub 2014 Sep 2. PubMed PMID: 25185215. 3: Martinel Lamas DJ, Carabajal E, Prestifilippo JP, Rossi L, Elverdin JC, Merani S, Bergoc RM, Rivera ES, Medina VA. Protection of radiation-induced damage to the hematopoietic system, small intestine and salivary glands in rats by JNJ7777120 compound, a histamine H4 ligand. PLoS One. 2013 Jul 26;8(7):e69106. doi: 10.1371/journal.pone.0069106. Print 2013. PubMed PMID: 23922686; PubMed Central PMCID: PMC3724844. 4: Coruzzi G, Pozzoli C, Adami M, Grandi D, Guido N, Smits R, de Esch I, Leurs R. Strain-dependent effects of the histamine H₄ receptor antagonist JNJ7777120 in a murine model of acute skin inflammation. Exp Dermatol. 2012 Jan;21(1):32-7. doi: 10.1111/j.1600-0625.2011.01396.x. PubMed PMID: 22151388. 5: Wagner E, Wittmann HJ, Elz S, Strasser A. Mepyramine-JNJ7777120-hybrid compounds show high affinity to hH(1)R, but low affinity to hH(4)R. Bioorg Med Chem Lett. 2011 Nov 1;21(21):6274-80. doi: 10.1016/j.bmcl.2011.09.001. Epub 2011 Sep 8. PubMed PMID: 21944853. 6: Seifert R, Schneider EH, Dove S, Brunskole I, Neumann D, Strasser A, Buschauer A. Paradoxical stimulatory effects of the "standard" histamine H4-receptor antagonist JNJ7777120: the H4 receptor joins the club of 7 transmembrane domain receptors exhibiting functional selectivity. Mol Pharmacol. 2011 Apr;79(4):631-8. doi: 10.1124/mol.111.071266. Epub 2011 Jan 25. Review. PubMed PMID: 21266488. 7: Rosethorne EM, Charlton SJ. Agonist-biased signaling at the histamine H4 receptor: JNJ7777120 recruits β-arrestin without activating G proteins. Mol Pharmacol. 2011 Apr;79(4):749-57. doi: 10.1124/mol.110.068395. Epub 2010 Dec 6. PubMed PMID: 21134907. 8: Zampeli E, Thurmond RL, Tiligada E. The histamine H4 receptor antagonist JNJ7777120 induces increases in the histamine content of the rat conjunctiva. Inflamm Res. 2009 Jun;58(6):285-91. doi: 10.1007/s00011-009-8245-4. PubMed PMID: 19184344. 9: Coruzzi G, Adami M, Guaita E, de Esch IJ, Leurs R. Antiinflammatory and antinociceptive effects of the selective histamine H4-receptor antagonists JNJ7777120 and VUF6002 in a rat model of carrageenan-induced acute inflammation. Eur J Pharmacol. 2007 Jun 1;563(1-3):240-4. Epub 2007 Feb 23. PubMed PMID: 17382315.