55476-47-6
55476-47-6 structure
- Name: PSB-12062
- Chemical Name: 10-(toluene-4-sulfonyl)-10H-phenoxazine
- CAS Number: 55476-47-6
- Molecular Formula: C19H15NO3S
- Molecular Weight: 337.39200
- Catalog: Signaling Pathways Membrane Transporter/Ion Channel P2X Receptor
- Create Date: 2018-06-14 11:51:31
- Modify Date: 2024-01-02 17:40:25
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PSB-12062 is a potent and selective P2X4 antagonist with an IC50 of 1.38 μM for human P2X4.
| Name | 10-(toluene-4-sulfonyl)-10H-phenoxazine |
|---|---|
| Synonyms |
PSB 12062
N-Tolylsulfonylphenoxazin PSB-12062 |
| Description | PSB-12062 is a potent and selective P2X4 antagonist with an IC50 of 1.38 μM for human P2X4. |
|---|---|
| Related Catalog | |
| Target |
IC50: 1.38 μM (human P2X4), 92.8 nM (rat P2X4), 1.76 μM (mouse P2X4)[1] |
| In Vitro | PSB-12062 shows similar potency in human, rat, and mouse species. PSB-12062 shows to be allosteric in nature with a 35-fold selectivity toward P2X4 versus P2X1, P2X2, P2X3, and P2X7. However, PSB-12062 is unable to completely block ATP-induced P2X4-mediated calcium influx even when used at high concentrations (>30 μM)[1]. |
| Kinase Assay | The competition binding studies are performed in assay buffer (50 mM Tris-HCl, pH 7.4) containing 1 mM EDTA and 0.2 nM [35S]ATPγS. The incubations are started by the addition of membranes (10-15 μg) and are performed in a 250 μL final assay volume. The reactions are terminated by vacuum filtration over GF/ B glass-fiber filters using a Brandell 48-well harvester. The filters are rinsed three times with ice-cold Tris-HCl buffer (50 mM, pH 7.4). The filters are punched out and transferred to 4 mL scintillation vials. Then 2.5 mL of Ultima Gold scintillation cocktail is added, and samples are counted after 6 h for 1 min each, using a liquid scintillation counter (LSC). Nonspecific binding of [35S]ATPγS is determined using 100 μM ATP[1]. |
| References |
| Molecular Formula | C19H15NO3S |
|---|---|
| Molecular Weight | 337.39200 |
| Exact Mass | 337.07700 |
| PSA | 54.99000 |
| LogP | 5.77350 |
| Storage condition | 2-8℃ |
