In Vivo (Add solvents to the product individually and in order.)
Homogeneous suspension
CMC-NA
≥5mg/ml
Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO
40%PEG300
5%Tween80
50%ddH2O
Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.
0.780mg/ml
(2.47mM)
Taking the 1 mL working solution as an example, add 50 μL of 15.6 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution
5% DMSO
95% Corn oil
Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.
0.525mg/ml
(1.66mM)
Taking the 1 mL working solution as an example, add 50 μL of 10.5 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
Biological Activity
Description
A-804598 is a selective P2X7R antagonist with high affinity at rat (IC50 = 10 nM), mouse (IC50 = 9 nM) and human (IC50 = 11 nM) P2X7 receptors.
Targets
rat P2X7R
rat P2X7R
human P2X7R
9 nM
10 nM
11 nM
In vitro
A-804598 represents a structurally novel, competitive, and selective antagonist that has equivalent high affinity at rat (IC50 = 10 nM), mouse (IC50 = 9 nM) and human (IC50 = 11 nM) P2X7 receptors. This compound also potently blocks agonist stimulated release of IL-1β(IC50 of 8.5 nM) and Yo-Pro uptake (IC50 of 8.1 nM) from differentiated THP-1 cells that natively express human P2X7 receptors. Although this compound potently blocks P2X7 receptor activation, at concentrations up to 100 μM, it does not significantly reduce agonist-evoked changes in intracellular calcium concentrations mediated by a variety of other P2X and P2Y receptors. This chemical shows weak or no activity for interating with a large array of G-protein-coupled receptors, enzymes, transporters, and ion channels (CEREP, Poitiers, France)(IC50 > 5-10 μM).
In Vivo
Inhibition of P2X7 through the antagonist A-804598 in SOD1-G93A mice suppresses SQSTM1/p62 up-regulation in lumbar spinal cord.
SOD1-G93A microglia are treated with 300 μM BzATP or 3 mM ATP for 15 min or 1 h with or without 10 μM A-804598 and subjected to western blotting and immunoreactions with anti-p-mTOR and anti-mTOR or anti-GAPDH.
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.
