General information
CAS n°
not found
Mechanism 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.
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