AZ 10606120 dihydrochloride |
| Catalog No.GC17375 |
Potent P2X7 receptor antagonist
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 607378-18-7
Sample solution is provided at 25 µL, 10mM.
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KD: 1.4 nM and 1.9 nM for human and rat P2X7 receptors, respectivley
The P2X7 receptor has intriguing biophysical properties, activates a diverse range of cellular events and mediates a wide range of functional effects. The P2X7 receptor is an ATP-gated ion channel known for its cytotoxic activity. However, recent evidence suggests a role for P2X7 in cell proliferation. AZ 10606120 is a P2X7 receptor antagonist.
In vitro: Binding of [3H]-AZ 10606120 was higher in membranes prepared from cells expressing P2X7 receptors than from control cells and was inhibited by ATP suggesting labelled sites represented human P2X7 receptors. Binding was reversible, saturable and modulated by P2X7 receptor ligands. The positive cooperativity observed suggests that binding of AZ 10606120 to one subunit in the P2X7 receptor complex enhances subsequent binding to other P2X7 subunits in the same complex. The negative cooperative effects of ATP suggest that ATP and AZ 10606120 bind at separate, interacting, sites on the P2X7 receptor [1].
In vivo: Intratumor injection of AZ10606120 caused a strong inhibition of tumor growth in B16-inoculated C57Bl/6 mice and caused in parallel a large reduction in VEGF staining and vessel formation [2].
Clinical trial: Up to now, AZ 10606120 is still in the preclinical development stage.
Reference:
[1] AD Michel, LJ Chambers, WC Clay, JP Condreay, DS Walter and IP Chessell. Direct labelling of the human P2X7 receptor and identification of positive and negative cooperativity of binding. British Journal of Pharmacology (2007) 151, 84–95
[2] Elena Adinolfi, Lizzia Raffaghello, Anna Lisa Giuliani, Luigi Cavazzini, Marina Capece, Paola Chiozzi, Giovanna Bianchi, Guido Kroemer, Vito Pistoia, and Francesco Di Virgilio. Expression of P2X7 Receptor Increases In Vivo Tumor Growth. Cancer Res; 72(12); 2957–69.
| Cas No. | 607378-18-7 | SDF | |
| Chemical Name | (Z)-2-((3r,5r,7r)-adamantan-1-yl)-N-((E)-2-((2-((2-hydroxyethyl)amino)ethyl)imino)-1,2-dihydroquinolin-5-yl)acetimidic acid dihydrochloride | ||
| Canonical SMILES | OCCNCC/N=C1C=CC2=C(N\1)C=CC=C2/N=C(O)/CC34C[C@@]5([H])C[C@](C3)([H])C[C@](C4)([H])C5.Cl.Cl | ||
| Formula | C25H34N4O2.2HCl | M.Wt | 495.48 |
| Solubility | <12.39mg/ml in Water; <49.55mg/ml in DMSO | Storage | Desiccate at RT |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.0182 mL | 10.0912 mL | 20.1824 mL |
| 5 mM | 0.4036 mL | 2.0182 mL | 4.0365 mL |
| 10 mM | 0.2018 mL | 1.0091 mL | 2.0182 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
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.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 6 reference(s) in Google Scholar.)
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