AZ10606120 (dihydrochloride)

AZ10606120 dihydrochloride is a selective, high affinity antagonist for P2X7 receptor (P2X7R) at human and rat with an IC₅₀ of about 10 nM. AZ10606120 dihydrochloride is little or no effect at other P2XR subtypes. AZ10606120 dihydrochloride has anti-depressant effects and reduces tumour growth^[1]. IC50 & Target:IC50: about 10 nM (P2X7R)^[1] In Vitro:AZ10606120 (1-100 μM, 72 h) dihydrochloride depletes tumour cells in patient-derived primary glioblastoma samples^[2].
AZ10606120 (1-100 μM, 72 h) dihydrochloride increases Lactate dehydrogenase (LDH) levels in human primary glioblastoma cultures^[2].
AZ10606120 (10 μM) dihydrochloride reduces proliferation (60 h), cell migration (1 h) and invasion (24 h) in PDAC cell lines^[3].
In Vivo:AZ10606120 (100 μg/kg, i.p., every 2 days for additional 15 days) dihydrochloride reverses Streptozotocin (HY-13753)-induced VEGF and IL-6 expression in the retinae of rats^[4].
AZ10606120 (2 mg/kg i.p.) dihydrochloride shows an antidepressant phenotype in LPS-induced anhedonia mice^[5].
AZ10606120 (5 mg/kg, i.m.) dihydrochloride and DNR (0.75 mg/kg, i.m.) combined administration is more effective in reducing HL-60 tumor growth in nude mice in comparison to their single administration^[6].