Home Neuronal Signaling P2 Receptor antagonist AZ10606120 dihydrochloride For research use only.

AZ10606120 dihydrochloride

Synonyms: AZ10606120 2HCl

AZ10606120 dihydrochloride (2HCl) is a potent and selective antagonist for P2X7 receptor (P2X7R) with IC50 of ~10 nM. AZ10606120 dihydrochloride exhibits anti-depressant effects and reduces tumour growth. This product is not soluble in PBS solution. Please do not dissolve it in PBS for administration.

AZ10606120 dihydrochloride Chemical Structure

AZ10606120 dihydrochloride Chemical Structure

CAS No. 607378-18-7

Purity & Quality Control

Batch: S352001 DMSO]99 mg/mL]false]Water]17 mg/mL]false]Ethanol]Insoluble]false Purity: 99.11%
99.11

AZ10606120 dihydrochloride Related Products

Signaling Pathway

P2 Receptor Signaling Pathways

P2 Receptor Signaling Pathway

Biological Activity

Description AZ10606120 dihydrochloride (2HCl) is a potent and selective antagonist for P2X7 receptor (P2X7R) with IC50 of ~10 nM. AZ10606120 dihydrochloride exhibits anti-depressant effects and reduces tumour growth. This product is not soluble in PBS solution. Please do not dissolve it in PBS for administration.
Targets
P2X7R [1]
(Cell-free assay)
10 nM
In vitro
In vitro

AZ10606120, a P2X7R antagonist, significantly reduces the tumour cell number in both U251 cells and human glioma samples, also more effectively inhibits tumour proliferation in U251 cells when compared with the conventional chemotherapeutic agent, temozolomide.[2]
Cell Research Cell lines Glioma cells from human tumour sample , U251 human glioblastoma cell line
Concentrations 5, 25 μM for U251 cells, 15 μM for human glioma samples
Incubation Time 72 h
Method

AZ10606120 concentrations of 5 μM and 25 μM was for U251 cells and 15 μM was for human glioma samples. For comparison of P2X7R antagonism efficacy with conventional glioma treatment, cells were also treated with the chemotherapeutic agent, temozolomide. After 72 h of treatment, cells were fixed with 1:1 acetone-methanol solution at − 20 °C for 15 min. Fixed cells were subsequently stained with 5 μM of DAPI nuclear counterstain at 25 °C for 1 h. Cells were viewed with an Olympus IX-81 fluorescence microscope, and a cell count was conducted based on the number of DAPI-positive nuclei.
In Vivo
In vivo

AZ10606120, the P2X7R allosteric inhibitor, has anti‐proliferative effects in vivo, by reducing pancreatic stellate cells (PSCs) number/activity and collagen deposition.[3]
Animal Research Animal Models Orthotopic xenograft mouse model of pancreatic ductal adenocarcinoma (PDAC)
Dosages 5 mg/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 495.48 Formula

C25H36Cl2N4O2
CAS No. 607378-18-7 SDF --
Smiles Cl.Cl.OCCNCCNC1=NC2=C(C=C1)C(=CC=C2)NC(=O)CC34CC5CC(CC(C5)C3)C4
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 99 mg/mL ( (199.8 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 17 mg/mL

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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