Molecular Formula | C14H16ClN3O |
Molar Mass | 277.75 |
Density | 1.322±0.06 g/cm3(Predicted) |
Boling Point | 477.0±45.0 °C(Predicted) |
Solubility | DMSO : 20 mg/mL mother liquor preservation: sub-package and freeze storage to avoid repeated freezing and thawing;-20 ℃,1 month;-80 ℃,6 months (after dilution, the solution temperature is low and storage may precipitate, try to use it now) Cell experiment: Dissolve with DMSO first: dilute with culture medium then, and the dilution process is recommended to be carried out in stages to avoid too fast concentration change leading to compound precipitation. If the compound is precipitated during the dilution process, it can be redissolved by ultrasound. During dilution, ensure that the final concentration of DMSO in the working fluid should be below 0.1% as far as possible, and the maximum should not exceed 0.5%, and set up a DMSO control group with corresponding concentration. Animal experiment: Dissolve with DMSO first: dilute with water or normal saline, etc. The dilution process is recommended to be carried out in sections to avoid excessive concentration changes leading to compound p |
Appearance | solid |
Color | white |
pKa | 15.20±0.30(Predicted) |
Storage Condition | room temp |
Use | JNJ-7777120 is the first, effective, selective non-imidazole histamine H4 receptor antagonist, Ki is 4.5 nM, which is more than 1000 times more selective than acting on other histamine receptors. |
Target | H4 receptor |
In vitro study | JNJ 7777120 binds to the H4 receptor with high affinity and is more than 1000 times more selective than other histamine receptors. JNJ 7777120 are potent, selective H4 receptor antagonists with little or no affinity for more than 50 other targets. |
In vivo study | The JNJ 7777120 has an oral bioavailability of 30% in treated rats and 100 in treated dogs, with a half-life of 3 hours for both breeds. 7777120 treatment of mouse bone marrow-derived mast cells with JNJ inhibits histamine-induced chemotaxis and calcium influx. Treatment of mice with JNJ 7777120 inhibits histamine-induced migration of tracheal mast cells from connective tissue to epithelial cells. JNJ 7777120 treatment of mouse zymosan-induced peritonitis model significantly inhibited neutrophil infiltration. |
Hazard Symbols | Xi - Irritant |
Risk Codes | 36/37/38 - Irritating to eyes, respiratory system and skin. |
Safety Description | S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S36 - Wear suitable protective clothing. |
WGK Germany | 3 |
Reference Show more | 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, b |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 3.6 ml | 18.002 ml | 36.004 ml |
5 mM | 0.72 ml | 3.6 ml | 7.201 ml |
10 mM | 0.36 ml | 1.8 ml | 3.6 ml |
5 mM | 0.072 ml | 0.36 ml | 0.72 ml |