Target nature :
unknown
CAS n° :
not found
Mecanism of action :
inhibition of cytokine production in cellular inflammatory model, in an acute lung inflammation model and in mouse pain model
Physico-chemical properties :
upon request
Probe availability :
Laboratory of therapeutic innovation, Illkirch
Princeps reference :
Bollenbach M., Salvat E., Daubeuf F., Wagner P., Yalcin I., Humo M., Letellier B., Becker LJ., Bihel F., Bourguignon JJ., Villa P., Obrecht A., Frossard N., Barrot M., M. Schmitt (2018) Phenylpyridine-2-ylguanidines and rigid mimetics as novel inhibitors of TNF¿ overproduction: Beneficial action in models of neuropathic pain and of acute lung inflammation. European Journal of Medicinal Chemistry 147: 163-182.
More bibliography :
Other available information on the probe :
White powder, stored at RT
Other information on the target :
available at LIT (Illkirch)
Selectivity profile :
not known
In vivo data :
Significative decrease after IP injection of 5 mg/kg (less than 50% of control) of neutrophils number, lymphcytes number and TNF release in an acute lung inflammation model.
Also active on a model of neuropathic pain (see Bollenbach et al)
In vitro data :
Inhibition of TNF alpha: IC50 = 1 µM +/- 0.1
inhibition of IL-1beta: IC50 = 3.7 µM +/- 0.2
Toxicity :
less than 20 % at 10 µM on human PBMC
Chaine SMILES :
N/C3=N/c2cc(c1ccccc1)ccc2CN3.Cl
Contact the author of the biotool
