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].

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

495.48

C₂₅H₃₆Cl₂N₄O₂

607378-18-7

Solid

White to off-white

O=C(NC1=C2C=CC(NCCNCCO)=NC2=CC=C1)CC3(C4)CC5CC4CC(C5)C3.[H]Cl.[H]Cl

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

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

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

• [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]