AZ-10606120 is a potent purinoceptor P2X7 negative allosteric modulator that antagonizes ATP-dependent P2X7 activation (IC50 against ATP-induced ethidium bromide uptake = 2.3 nM and 24 nM, respectively, using human or rat P2X7 HEK293 transfectants; [ATP] = EC50) in a non-competitive and slowly reversible manner via affinity interaction at an allosteric pocket (human/rat P2X7 KD = 1.4 nM/19 nM) distinct from the KN-62- or ATP-binding site. A useful tool for probing P2X7-mediated physiological and pathological processes both in cultures (0.1-10 µM) and in vivo (e.g. 5 mg/kg i.p., 300 nM i.m., or 3 µg i.c.v.; in mice).
Potent purinoceptor P2X7 negative allosteric modulator that antagonizes ATP-dependent P2X7 activation in a non-competitive and slowly reversible manner.
Il team dei nostri ricercatori vanta grande esperienza in tutte le aree della ricerca quali Life Science, scienza dei materiali, sintesi chimica, cromatografia, discipline analitiche, ecc..