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A-804598 is a competitive and selective P2X7 receptor antagonist (IC50: 10 nM, rat; 9 nM, mouse; 11 nM, human).
Pack Size | Price | Availability | Quantity |
---|---|---|---|
2 mg | $31 | In Stock | |
5 mg | $48 | In Stock | |
10 mg | $73 | In Stock | |
25 mg | $156 | In Stock | |
50 mg | $272 | In Stock | |
100 mg | $438 | In Stock | |
500 mg | $982 | In Stock | |
1 mL x 10 mM (in DMSO) | $53 | In Stock |
Description | A-804598 is a competitive and selective P2X7 receptor antagonist (IC50: 10 nM, rat; 9 nM, mouse; 11 nM, human). |
Targets&IC50 | P2X7R (human):11 nM, P2X7R (rat):10 nM, P2X7R (rat):9 nM |
In vitro | A-804598 effectively blocked IL-1β release in the THP-1 cells (IC50: 8.5 nM). It also blocked agonist-evoked pore formation in differentiated human THP-1 cells (IC50: 8.1 nM) with similar potency as in the calcium-influx assay. [1] |
In vivo | According to the autoradiographic analysis of coronal rat brain sections, there was specific binding of [3H]-A-804598 throughout the rat brain. In the grey matter of the L4-L6 region of the rat spinal cord, it was also found that high levels of [3H]-A-804598 specific binding. [2] |
Alias | A 804598 |
Molecular Weight | 315.37 |
Formula | C19H17N5 |
Cas No. | 1125758-85-1 |
Smiles | C[C@H](N(C(=N)NC#N)c1cccc2ncccc12)c1ccccc1 |
Relative Density. | 1.17 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 31.5 mg/mL (100 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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