Biological Activity
Potent P2X7 receptor antagonist (KD values are 1.4 and 19 nM at human and rat P2X7 receptors respectively). Binds in a positive cooperative manner to sites distinct from, but coupled to, the ATP binding site and acts as a negative allosteric modulator. Inhibits tumor growth and displays antiangiogenic effects in mice.
Licensing Information
Sold for research purposes under agreement from AstraZeneca
Compound Libraries
AZ 10606120 dihydrochloride is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 495.48 |
| Formula | C25H34N4O2.2HCl |
| Storage | Desiccate at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 607378-18-7 |
| PubChem ID | 56972227 |
| InChI Key | BVFONFUUWORSPO-UHFFFAOYSA-N |
| Smiles | O=C(NC4=C(C=CC(NCCNCCO)=N5)C5=CC=C4)CC1(C3)CC2CC(CC3C2)C1.Cl.Cl |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 49.55 | 100 | |
| water | 12.39 | 25 |
Preparing Stock Solutions
The following data is based on the product molecular weight 495.48. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.02 mL | 10.09 mL | 20.18 mL |
| 5 mM | 0.4 mL | 2.02 mL | 4.04 mL |
| 10 mM | 0.2 mL | 1.01 mL | 2.02 mL |
| 50 mM | 0.04 mL | 0.2 mL | 0.4 mL |
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References
References are publications that support the products' biological activity.
Michel et al (2007) Direct labelling of the human P2X7 receptor and identification of positive and negative cooperativity of binding. Br.J.Pharmacol. 151 103 PMID: 17339830
Michel and Fonfria (2007) Agonist potency at P2X7 receptors is modulated by structurally diverse lipids. Br.J.Pharmacol. 152 523 PMID: 17700717
Michel et al (2008) Negative and positive allosteric modulators of the P2X7 receptor. Br.J.Pharmacol. 153 737 PMID: 18071294
Adinolfi et al (2012) Expression of P2X7 receptor increases in vivo tumor growth. Cancer Res. 72 2957 PMID: 22505653
Keywords: AZ 10606120 dihydrochloride, supplier, Potent, P2X7, receptor, antagonists, Receptors, Purinergic, purinoceptors, AZ10606120, dihydrochloride, AstraZeneca, P2X, Receptors, P2X, Receptors, Tocris Bioscience
