WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 522409
CAS#: 459168-41-3
Description: 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.
MedKoo Cat#: 522409
Name: JNJ7777120
CAS#: 459168-41-3
Chemical Formula: C14H16ClN3O
Exact Mass: 277.09819
Molecular Weight: 277.75
Elemental Analysis: C, 60.54; H, 5.81; Cl, 12.76; N, 15.13; O, 5.76
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
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 |
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.
