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].

Product Specifications

CAS Number

[607378-18-7]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

P2X Receptor

Type

Reference compound

Related Pathways

Membrane Transporter/Ion Channel

Applications

Cancer-programmed cell death

Field of Research

Cancer; Neurological Disease

Assay Protocol

https://www.medchemexpress.com/az10606120-dihydrochloride.html

Purity

99.93

Solubility

DMSO : 8.33 mg/mL (ultrasonic) |H2O : 2 mg/mL (ultrasonic)

Smiles

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

Molecular Formula

C25H36Cl2N4O2

Molecular Weight

495.48

Precautions

H302, H315, H319, H335

References & Citations

[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.|[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. |[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.|[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. |[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.|[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.