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AZ10606120 dihydrochloride

MCE China：AZ10606120 dihydrochloride

Brand：MedChemExpress (MCE)

Cat. No.HY-108669

CAS：607378-18-7

Purity：99.38%

Storage：4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Shipping：Room temperature in continental US; may vary elsewhere.

Description：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.

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].

IC50 & Target：P2X7 Receptor

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References：

[1]. Allsopp RC, et al. Unique residues in the ATP gated human P2X7 receptor define a novel allosteric binding pocket for the selective antagonist AZ10606120. Sci Rep. 2017 Apr 7;7(1):725.  [Content Brief]

[2]. Kan LK, et al. P2X7 receptor antagonism by AZ10606120 significantly reduced in vitro tumour growth in human glioblastoma. Sci Rep. 2023 May 24;13(1):8435.  [Content Brief]

[3]. Giannuzzo A, et al. The P2X7 receptor regulates cell survival, migration and invasion of pancreatic ductal adenocarcinoma cells. Mol Cancer. 2015 Nov 25;14:203.  [Content Brief]

[4]. Clapp C, et al. Pharmacological blockade of the P2X7 receptor reverses retinal damage in a rat model of type 1 diabetes. Acta Diabetol. 2019 Sep;56(9):1031-1036.  [Content Brief]

[5]. Csölle C, et al. Neurochemical Changes in the Mouse Hippocampus Underlying the Antidepressant Effect of Genetic Deletion of P2X7 Receptors. PLoS One. 2013 Jun 21;8(6):e66547.  [Content Brief]

[6]. Pegoraro A, et al. Differential sensitivity of acute myeloid leukemia cells to daunorubicin depends on P2X7A versus P2X7B receptor expression. Cell Death Dis. 2020 Oct 18;11(10):876.  [Content Brief]