Powder: -20°C for 3 years | In solvent: -80°C for 1 year
JNJ-47965567 (JNJ-479655) is a selective antagonist of the purinergic receptor P2X subtype 7 (P2X7), a ligand-gated ion channel(with pKis of 7.9 and 8.7 for human and rat P2X7, respectively).
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 34.00 | |
2 mg | In stock | $ 48.00 | |
5 mg | In stock | $ 80.00 | |
10 mg | In stock | $ 159.00 | |
25 mg | In stock | $ 318.00 | |
50 mg | In stock | $ 475.00 | |
100 mg | In stock | $ 678.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 87.00 |
Description | JNJ-47965567 (JNJ-479655) is a selective antagonist of the purinergic receptor P2X subtype 7 (P2X7), a ligand-gated ion channel(with pKis of 7.9 and 8.7 for human and rat P2X7, respectively). |
Targets&IC50 | P2X7 (human):7.9(pKis), P2X7 (rat):8.7(pKis) |
In vitro | JNJ-47965567 is potent high affinity (pKi 7.9 0.07), selective human P2X7 antagonist, with no significant observed speciation.?In native systems, the potency of the compound to attenuate IL-1β release was 6.7 0.07 (human blood), 7.5 0.07 (human monocytes) and 7.1 0.1 (rat microglia).?JNJ-47965567 exhibited target engagement in rat brain, with a brain EC50 of 78 19 ng·mL(-1) (P2X7 receptor autoradiography) and functional block of Bz-ATP induced IL-1β release.?JNJ-47965567 (30 mg·kg(-1) ) attenuated amphetamine-induced hyperactivity and exhibited modest, yet significant efficacy in the rat model of neuropathic pain.?No efficacy was observed in forced swim test. |
Animal Research | The authors used a combination of in vitro assays (calcium flux, radioligand binding, electrophysiology, IL-1β release) in both recombinant and native systems.?Target engagement of JNJ-47965567 was demonstrated by ex vivo receptor binding autoradiography and in vivo blockade of Bz-ATP induced IL-1β release in the rat brain.?Finally, the efficacy of JNJ-47965567 was tested in standard models of depression, mania and neuropathic pain |
Synonyms | JNJ-479655 |
Molecular Weight | 488.64 |
Formula | C28H32N4O2S |
CAS No. | 1428327-31-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 200 mg/mL (409.30 mM), Sonification is recommended.
You can also refer to dose conversion for different animals. More
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JNJ-47965567 1428327-31-4 Membrane transporter/Ion channel Neuroscience P2X Receptor Inhibitor P2X7 JNJ479655 JNJ 47965567 pain JNJ47965567 JNJ-479655 inhibit JNJ 479655 neuropathic P2XRs inhibitor